-
1
-
-
77951065603
-
-
Uniting the world against AIDS Accessed December 2009
-
Uniting the world against AIDS. AIDS epidemic update 2009. http://www.unaids.org/en/(Accessed December 2009)
-
AIDS Epidemic Update 2009
-
-
-
2
-
-
61449189645
-
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV
-
De Clercq, E. Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int. J. Antimicrob. Agentsl., 2009, 33, 307-320.
-
(2009)
Int. J. Antimicrob. Agentsl.
, vol.33
, pp. 307-320
-
-
De Clercq, E.1
-
3
-
-
36749073433
-
The design of drugs for HIV and HCV
-
DOI 10.1038/nrd2424, PII NRD2424
-
De Clercq, E. The design of drugs for HIV and HCV. Nat. Rev. Drug. Discov., 2007, 6, 1001-1018. (Pubitemid 350213865)
-
(2007)
Nature Reviews Drug Discovery
, vol.6
, Issue.12
, pp. 1001-1018
-
-
De Clercq, E.1
-
4
-
-
43049106403
-
Novel HIV-1 reverse transcriptase inhibitors
-
Jochmans, D. Novel HIV-1 reverse transcriptase inhibitors. Virus. Res., 2008, 134, 171-185.
-
(2008)
Virus. Res.
, vol.134
, pp. 171-185
-
-
Jochmans, D.1
-
5
-
-
32644438459
-
Dawn of non-nucleoside inhibitor-based anti-HIV microbicides
-
DOI 10.1093/jac/dki464
-
D'Cruz, O. J.; Uckun, F. M. Dawn of non-nucleoside inhibitor-based anti- HIV microbicides. J. Antimicrob. Chemother., 2006, 57(3), 411-423. (Pubitemid 43240192)
-
(2006)
Journal of Antimicrobial Chemotherapy
, vol.57
, Issue.3
, pp. 411-423
-
-
D'Cruz, O.J.1
Uckun, F.M.2
-
6
-
-
0029075207
-
Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors
-
Ding, J.; Das, K.; Moereels, H.; Koymans, L.; Andries, K.; Janssen, P. A. J.; Hughes, S. H.; Arnold, E. Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors. Nat. Struct. Biol., 1995, 2, 407-415.
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 407-415
-
-
Ding, J.1
Das, K.2
Moereels, H.3
Koymans, L.4
Andries, K.5
Janssen, P.A.J.6
Hughes, S.H.7
Arnold, E.8
-
7
-
-
0028947588
-
High resolution structures of HIV-1 RT from four RT-inhibitor complexes
-
Ren, J.; Esnouf, R.; Garman, E.; Somers, D.; Ross, C.; Kirby, I.; Keeling, J.; Darby, G.; Jones, Y.; Stuart, D. High resolution structures of HIV-1 RT from four RT-inhibitor complexes. Nat. Struct. Biol., 1995, 2, 293-302.
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 293-302
-
-
Ren, J.1
Esnouf, R.2
Garman, E.3
Somers, D.4
Ross, C.5
Kirby, I.6
Keeling, J.7
Darby, G.8
Jones, Y.9
Stuart, D.10
-
8
-
-
0024832408
-
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative
-
DOI 10.1016/0006-291X(89)92756-3
-
M. Baba, H. Tanaka, E. De Clercq, R. Pauwels, J. Balzarini, D. Schols, H. Nakashima, C.F. Perno, R.T. Walker, T. Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. Miyasaka, Biochem. Biophys. Res. Commun., 1989, 165, 1375-1381. (Pubitemid 20029862)
-
(1989)
Biochemical and Biophysical Research Communications
, vol.165
, Issue.3
, pp. 1375-1381
-
-
Baba, M.1
Tanaka, H.2
De Clercq, E.3
Pauwels, R.4
Balzarini, J.5
Schols, D.6
Nakashima, H.7
Perno, C.-F.8
Walker, R.T.9
Miyasaka, T.10
-
9
-
-
0032918170
-
Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection
-
DOI 10.1016/S0014-827X(98)00103-7, PII S0014827X98001037
-
De Clercq, E. Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection. Farmaco, 1999, 54, 26-45. (Pubitemid 29187015)
-
(1999)
Farmaco
, vol.54
, Issue.1-2
, pp. 26-45
-
-
De Clercq, E.1
-
10
-
-
0036104758
-
Non-nucleoside HIV-1 reverse transciptase (RT) inhibitors: Past, present, and future perspectives
-
Campiani, G.; Ramunno, A.; Maga, G.; Nacci, V.; Fattorusso, C.; Catalanotti, B.; Morelli, E.; Novellino, E. Non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors: past, present, and future perspectives. Curr. Pharm Des., 2002, 8, 615-657. (Pubitemid 34406406)
-
(2002)
Current Pharmaceutical Design
, vol.8
, Issue.8
, pp. 615-657
-
-
Campiani, G.1
Ramunno, A.2
Maga, G.3
Nacci, V.4
Fattorusso, C.5
Catalanotti, B.6
Morelli, E.7
Novellino, E.8
-
11
-
-
62749200513
-
Drug resistance mutations for surveillance of transmitted hiv-1 drug-resistance
-
Bennett, D. E.; Camacho, R. J.; Otelea, D.; Kuritzkes, D. R.; Fleury, H.; Kiuchi, M.; Heneine, W.; Kantor, R.; Jordan, M. R.; Schapiro, J. M.; Vandamme, A. M.; Sandstrom, P.; Boucher, C. A.; van de Vijver, D.; Rhee, S. Y.; Liu, T. F.; Pillay, D.; Shafer, R. W. Drug Resistance Mutations for Surveillance of Transmitted HIV-1 Drug-Resistance. PLoS One. 2009, 4(3):e4724.
-
(2009)
PLoS One.
, vol.4
, Issue.3
-
-
Bennett, D.E.1
Camacho, R.J.2
Otelea, D.3
Kuritzkes, D.R.4
Fleury, H.5
Kiuchi, M.6
Heneine, W.7
Kantor, R.8
Jordan, M.R.9
Schapiro, J.M.10
Vandamme, A.M.11
Sandstrom, P.12
Boucher, C.A.13
Van De Vijver, D.14
Rhee, S.Y.15
Liu, T.F.16
Pillay, D.17
Shafer, R.W.18
-
12
-
-
77949324191
-
Update of the drug resistance mutations in HIV-1: December 2009
-
Johnson, V. A.; Brun-Vezinet, F.; Clotet, B.; Gunthard, H. F.; Kuritzkes, D. R.; Pillay, D.; Schapiro, J. M.; Richman, D. D. Update of the drug resistance mutations in HIV-1: December 2009. Top HIV Med., 2009, 17(5), 138-145.
-
(2009)
Top HIV Med.
, vol.17
, Issue.5
, pp. 138-145
-
-
Johnson, V.A.1
Brun-Vezinet, F.2
Clotet, B.3
Gunthard, H.F.4
Kuritzkes, D.R.5
Pillay, D.6
Schapiro, J.M.7
Richman, D.D.8
-
13
-
-
33748500440
-
Novel tight binding PETT, HEPT and DABO-based non-nucleoside inhibitors of HIV-1 reverse transcriptase
-
DOI 10.1080/14756360600774413, PII UH5216760405L724
-
D'Cruz, O. J.; Uckun, F. M. Novel tight binding PETT, HEPT and DABObased non-nucleoside inhibitors of HIV-1 reverse transcriptase. J. Enzyme Inhib. Med. Chem., 2006, 21 (4), 329-350. (Pubitemid 44355782)
-
(2006)
Journal of Enzyme Inhibition and Medicinal Chemistry
, vol.21
, Issue.4
, pp. 329-350
-
-
D'Cruz, O.J.1
Uckun, F.M.2
-
14
-
-
73549088708
-
Molecular basis of human immunodeficiency virus drug resistance: An update
-
Menéndez-Arias, L. Molecular basis of human immunodeficiency virus drug resistance: An update. Antiviral Res., 2010, 85(1), 210-231.
-
(2010)
Antiviral Res.
, vol.85
, Issue.1
, pp. 210-231
-
-
Menéndez-Arias, L.1
-
15
-
-
54849438319
-
Substrate-induced stable enzyme-inhibitor complex formation allows tight binding of novel 2-aminopyrimidin-4(3H)-ones to drug-resistant HIV-1 reverse transcriptase mutants
-
Samuele, A.; Facchini, M.; Rotili, D.; Mai, A.; Artico, M.; Armand-Ugón, M.; Esté, J. A.; Maga, G. Substrate-induced stable enzyme-inhibitor complex formation allows tight binding of novel 2-aminopyrimidin-4(3H)-ones to drug-resistant HIV-1 reverse transcriptase mutants. Chem. Med. Chem., 2008, 3(9), 1412-1418.
-
(2008)
Chem. Med. Chem.
, vol.3
, Issue.9
, pp. 1412-1418
-
-
Samuele, A.1
Facchini, M.2
Rotili, D.3
Mai, A.4
Artico, M.5
Armand-Ugón, M.6
Esté, J.A.7
Maga, G.8
-
16
-
-
13844316071
-
5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin- 4(3H) -ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family
-
DOI 10.1016/j.bmc.2005.01.005
-
Mai, A.; Artico, M.; Ragno, R.; Sbardella, G.; Massa, S.; Musiu, C.; Mura, M.; Marturana, F.; Cadeddu, A.; Maga, G.; La Colla, P. 5-Alkyl-2- alkylamino-6-(2,6- difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family. Bioorg. Med. Chem., 2005, 13, 2065-2077. (Pubitemid 40261127)
-
(2005)
Bioorganic and Medicinal Chemistry
, vol.13
, Issue.6
, pp. 2065-2077
-
-
Mai, A.1
Artico, M.2
Ragno, R.3
Sbardella, G.4
Massa, S.5
Musiu, C.6
Mura, M.7
Marturana, F.8
Cadeddu, A.9
Maga, G.10
La Colla, P.11
-
17
-
-
0027521797
-
3,4-dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs): A new class of specific inhibitors of human immunodeficiency virus Type 1
-
Artico, M.; Massa, S.; Mai, A.; Marongiu, M. E.; Piras, G.; Tramontano, E.; La Colla, P. 3,4-Dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs): A New Class of Specific Inhibitors of Human Immunodeficiency Virus Type 1. Antiviral Chem. Chemother., 1993, 4, 361-368. (Pubitemid 23341334)
-
(1993)
Antiviral Chemistry and Chemotherapy
, vol.4
, Issue.6
, pp. 361-368
-
-
Artico, M.1
Massa, S.2
Mai, A.3
Marongiu, M.E.4
Piras, G.5
Tramontano, E.6
La Colla, P.7
-
18
-
-
0028522917
-
Characterization of the anti-hiv-1 activity of 3,4-dihydro-2-alkoxy-6- benzyl-4-oxopyrimidines (dabos), new non- nucleoside reverse transcriptase inhibitors
-
Tramontano, E.; Marongiu, M. E.; De Montis, A.; Loi, A. G.;Artico, M.; Massa, S.; Mai, A.; La Colla, P. Characterization of the Anti-HIV-1 Activity of 3,4-Dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs), New Non- Nucleoside Reverse Transcriptase Inhibitors. New Microbiol., 1994, 17, 269-279.
-
(1994)
New Microbiol.
, vol.17
, pp. 269-279
-
-
Tramontano, E.1
Marongiu, M.E.2
De Montis, A.3
Loi, A.G.4
Artico, M.5
Massa, S.6
Mai, A.7
La Colla, P.8
-
19
-
-
0028869436
-
Synthesis and antiviral activity of new 3,4-dihydro- 2-alkoxy- 6-benzyl-4-oxopyrimidines (dabos), specific inhibitors of human immunodeficiency virus type-1
-
Massa, S.; Mai, A.; Artico, M.; Sbardella, G.; Tramontano, E.;Loi, A. G.; Scano, P.; La Colla, P. Synthesis and Antiviral Activity of New 3,4-Dihydro- 2-alkoxy- 6-benzyl-4-oxopyrimidines (DABOs), Specific Inhibitors of Human Immunodeficiency Virus Type-1. Antivir. Chem. Chemother., 1995, 6, 1-8.
-
(1995)
Antivir. Chem. Chemother.
, vol.6
, pp. 1-8
-
-
Massa, S.1
Mai, A.2
Artico, M.3
Sbardella, G.4
Tramontano, E.5
Loi, A.G.6
Scano, P.7
La Colla, P.8
-
20
-
-
10744230514
-
Computer-Aided Design, Synthesis, and Anti-HIV-1 Activity in Vitro of 2-Alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H) -ones as Novel Potent Non-Nucleoside Reverse Transcriptase Inhibitors, Also Active Against the Y181C Variant
-
DOI 10.1021/jm0309856
-
Ragno, R.; Mai, A.; Sbardella, G.; Artico, M.; Massa, S.; Musiu, C.; Mura, M.; Marturana, F.; Cadeddu, A.; La Colla, P. Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6- difluorophenyl)alkyl]-3,4- dihydro-5- alkylpyrimidin- 4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant. J. Med. Chem., 2004, 47, 928-934. (Pubitemid 38176795)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.4
, pp. 928-934
-
-
Ragno, R.1
Mai, A.2
Sbardella, G.3
Artico, M.4
Massa, S.5
Musiu, C.6
Mura, M.7
Marturana, F.8
Cadeddu, A.9
La Colla, P.10
-
21
-
-
0029095334
-
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyl oxopyrimidines
-
Mai, A.; Artico, M.; Sbardella, G.; Massa, S.; Loi, A. G.; Tramontano, E.; Scano, P.; La Colla, P. Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyl oxopyrimidines. J. Med. Chem., 1995, 38, 3258-3263.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 3258-3263
-
-
Mai, A.1
Artico, M.2
Sbardella, G.3
Massa, S.4
Loi, A.G.5
Tramontano, E.6
Scano, P.7
La Colla, P.8
-
22
-
-
15444340492
-
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: Novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series
-
DOI 10.1021/jm960802y
-
Mai, A.; Artico, M.; Sbardella, G.; Quartarone, S.; Massa, S.; Loi, A.G.; De Montis, A.; Scintu, F.; Putzolu, M.; La Colla, P. Dihydro(alkylthio)- (naphthylmethyl)oxopyrimidines: Novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. J. Med. Chem., 1997, 40, 1447-1454. (Pubitemid 27200761)
-
(1997)
Journal of Medicinal Chemistry
, vol.40
, Issue.10
, pp. 1447-1454
-
-
Mai, A.1
Artico, M.2
Sbardella, G.3
Quartarone, S.4
Massa, S.5
Loi, A.G.6
De Montis, A.7
Scintu, F.8
Putzolu, M.9
La Colla, P.10
-
23
-
-
0029976422
-
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent nonnucleoside inhibitors
-
Hopkins, A. L.; Ren, J.; Esnouf, R. M.; Willcox, B. E.; Jones, E. Y.; Ross, C.; Miyasaka, T.; Walker, R. T.; Tanaka, H.; Stammers, D. K.; Stuart, D. I. Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent nonnucleoside inhibitors. J. Med. Chem., 1996, 39, 1589-1600.
-
(1996)
J. Med. Chem.
, vol.39
, pp. 1589-1600
-
-
Hopkins, A.L.1
Ren, J.2
Esnouf, R.M.3
Willcox, B.E.4
Jones, E.Y.5
Ross, C.6
Miyasaka, T.7
Walker, R.T.8
Tanaka, H.9
Stammers, D.K.10
Stuart, D.I.11
-
24
-
-
0033602141
-
5-alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin- 4(3H)-ones: Novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives
-
DOI 10.1021/jm980260f
-
Mai, A.; Artico, M.; Sbardella, G.; Massa, S.; Novellino, E.; Greco, G.; Loi, A. G.; Tramontano, E.; Marongiu, M. E.; La Colla, P. 5-Alkyl-2-alkylthio-6- (2,6- dihalophenyl-methyl)-3,4-dihydropyrimidin- 4(3H)-ones: Novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives. J. Med. Chem., 1999, 42, 619-627. (Pubitemid 29110778)
-
(1999)
Journal of Medicinal Chemistry
, vol.42
, Issue.4
, pp. 619-627
-
-
Mai, A.1
Artico, M.2
Sbardella, G.3
Massa, S.4
Novellino, E.5
Greco, G.6
Loi, A.G.7
Tramontane, E.8
Marongiu, M.E.9
La Colla, P.10
-
25
-
-
0028329454
-
Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro
-
Baba, M.; Shigeta, S.; Yuasa, S.; Takashima, H.; Sekiya, K.; Ubasawa, M.; Tanaka, H.; Miyasaka, T.; Walker, R. T.; De Clercq, E. Preclinical Evaluation of MKC-442, a Highly Potent and Specific Inhibitor of Human Immunodeficiency Virus Type 1 in vitro. Antimicrob. Agents Chemother., 1994, 38, 688-692. (Pubitemid 24114002)
-
(1994)
Antimicrobial Agents and Chemotherapy
, vol.38
, Issue.4
, pp. 688-692
-
-
Baba, M.1
Shigeta, S.2
Yuasa, S.3
Takashima, H.4
Sekiya, K.5
Ubasawa, M.6
Tanaka, H.7
Miyasaka, T.8
Walker, R.T.9
De Clercq, E.10
-
26
-
-
0025679303
-
Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor
-
Merluzzi, V. J.; Hargrave, K. D.; Labadia, M.; Grozinger, K.;Skoog, M.; Wu, J. C.; Shih, C. K.; Eckner, K.; Hattox, S.; Adams, J.; Rosenthal, A. S.; Faanes, R.; Eckner, R. J.; Koup, R. A.; Sullivan, J. L. Inhibition of HIV-1 Replication by a Nonnucleoside Reverse Transcriptase Inhibitor. Science, 1990, 250, 1411-1413. (Pubitemid 120031860)
-
(1990)
Science
, vol.250
, Issue.4986
, pp. 1411-1413
-
-
Merluzzi, V.J.1
Hargrave, K.D.2
Labadia, M.3
Grozinger, K.4
Skoog, M.5
Wu, J.C.6
Shih, C.-K.7
Eckner, K.8
Hattox, S.9
Adams, J.10
Rosehthal, A.S.11
Faanes, R.12
Eckner, R.J.13
Koup, R.A.14
Sullivan, J.L.15
-
27
-
-
0035797356
-
3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
-
DOI 10.1021/jm010853h
-
Mai, A.; Sbardella, G.; Artico, M.; Ragno, R.; Massa, S.; Novellino, E.; Greco, G.; Lavecchia, A.; Musiu, C.; La Colla, M.; Murgioni, C.; La Colla, P.; Loddo, R. Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6- difluorophenyl)alkyl]- 3,4-dihydro-5- alkylpyrimidin-4(3H)-ones as nonnucleoside inhibitors of HIV-1 reverse transcriptase. J. Med. Chem., 2001, 44, 2544-2554. (Pubitemid 32852144)
-
(2001)
Journal of Medicinal Chemistry
, vol.44
, Issue.16
, pp. 2544-2554
-
-
Mai, A.1
Sbardella, G.2
Artico, M.3
Ragno, R.4
Massa, S.5
Novellino, E.6
Greco, G.7
Lavecchia, A.8
Musiu, C.9
La Colla, M.10
Murgioni, C.11
La Colla, P.12
Loddo, R.13
-
28
-
-
29144440875
-
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity
-
DOI 10.1021/jm050744t
-
Manetti, F.; Esté, J. A.; Clotet-Codina, I.; Armand-Ugón, M.; Maga, G.; Crespan, E.; Cancio, R.; Mugnaini, C.; Bernardini, C.; Togninelli, A.; Carmi, C.; Alongi, M.; Petricci, E.; Massa, S.; Corelli, F.; Botta, M. Parallel Solution-Phase and Microwave-Assisted Synthesis of New S-DABO Derivatives Endowed with Subnanomolar Anti-HIV-1 Activity. J. Med. Chem., 2005, 48, 8000-8008. (Pubitemid 41798430)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.25
, pp. 8000-8008
-
-
Manetti, F.1
Este, J.A.2
Clotet-Codina, I.3
Armand-Ugon, M.4
Maga, G.5
Crespan, E.6
Cancio, R.7
Mugnaini, C.8
Bernardini, C.9
Togninelli, A.10
Carmi, C.11
Alongi, M.12
Petricci, E.13
Massa, S.14
Corelli, F.15
Botta, M.16
-
29
-
-
28544446294
-
Solution-phase parallel synthesis of S-DABO analogues
-
DOI 10.1016/j.tetlet.2005.10.142, PII S0040403905023981
-
Togninelli, A.; Carmi, C.; Petricci, E.; Mugnain,i C.; Massa, S.; Corelli, F.; Botta, M. Solution-phase parallel synthesis of S-DABO analogues. Tetrahedron Letters, 2006, 47, 65-67. (Pubitemid 41743778)
-
(2006)
Tetrahedron Letters
, vol.47
, Issue.1
, pp. 65-67
-
-
Togninelli, A.1
Carmi, C.2
Petricci, E.3
Mugnaini, C.4
Massa, S.5
Corelli, F.6
Botta, M.7
-
30
-
-
60549105209
-
Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethylsubstituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors
-
Wang, Y. P.; Chen. F. E.; De Clercq, E.; Balzarini, J.; Pannecouque, C. Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethylsubstituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors. Eur. J. Med. Chem., 2009, 44, 1016-1023.
-
(2009)
Eur. J. Med. Chem.
, vol.44
, pp. 1016-1023
-
-
Wang, Y.P.1
Chen, F.E.2
De Clercq, E.3
Balzarini, J.4
Pannecouque, C.5
-
31
-
-
2442610540
-
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series
-
DOI 10.1016/j.bmcl.2004.04.008, PII S0960894X04004895
-
He, Y.; Chen, F.; Sun, G.; Wang, Y.; De Clercq, E.; Balzarini, J.; Pannecouque, C. 5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1- naphthylmethyl) pyrimidin- 4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. Bioorg. Med. Chem. Lett., 2004, 14, 3173-3176. (Pubitemid 38624587)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.12
, pp. 3173-3176
-
-
He, Y.1
Chen, F.2
Sun, G.3
Wang, Y.4
De Clercq, E.5
Balzarini, J.6
Pannecouque, C.7
-
32
-
-
8644248445
-
Nonnucleoside HIV-1 reverse transcriptase inhibitors; Part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxyl-carbonylmethyl)thio]-6- (1- naphthylmethyl) pyrimidin-4(3H)-ones
-
DOI 10.1016/j.bioorg.2004.05.007, PII S0045206804000355
-
He, Y.; Chen, F.; Yu, X.; Wang, Y.; De Clercq, E.; Balzarini, J.; Pannecouque, C. Nonnucleoside HIV-1 reverse transcriptase inhibitors; part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxylcarbonylmethyl) thio]-6-(1-naphthylmethyl)pyrimidin-4(3H)-ones. Bioorg. Chem., 2004, 32, 536-548. (Pubitemid 39504948)
-
(2004)
Bioorganic Chemistry
, vol.32
, Issue.6
, pp. 536-548
-
-
He, Y.1
Chen, F.2
Yu, X.3
Wang, Y.4
De Clercq, E.5
Balzarini, J.6
Pannecouque, C.7
-
33
-
-
0035139222
-
SJ-3366, a unique and highly potent nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1) that also inhibits HIV-2
-
DOI 10.1128/AAC.45.2.393-400.2001
-
Buckheit, R.W. Jr.; Watson, K.; Fliakas-Boltz, V.; Russell, J.; Loftus, T. L.; Osterling, M. C.; Turpin, J. A.; Pallansch, L. A.; White, E.L.; Lee, J. W.; Lee, S. H.; Oh, J. W.; Kwon, H. S.; Chung, S. G.; Cho, E.H. SJ-3366, a unique and highly potent nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1) that also inhibits HIV-2. Antimicrob. Agents Chemother, 2001, 45, 393-400. (Pubitemid 32106715)
-
(2001)
Antimicrobial Agents and Chemotherapy
, vol.45
, Issue.2
, pp. 393-400
-
-
Buckheit Jr., R.W.1
Watson, K.2
Fliakas-Boltz, V.3
Russell, J.4
Loftus, T.L.5
Osterling, M.C.6
Turpin, J.A.7
Pallansch, L.A.8
White, E.L.9
Lee, J.-W.10
Lee, S.-H.11
Oh, J.-W.12
Kwon, H.-S.13
Chung, S.-G.14
Cho, E.-H.15
-
34
-
-
41649106236
-
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
-
DOI 10.1016/j.bmc.2008.01.039, PII S0968089608000576
-
Wang, Y. P.; Chen, F. E.; De Clercq, E.; Balzarini, J.; Pannecouque, C. Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2- (arylcarbonylmethylthio) pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg. Med. Chem., 2008, 16, 3887-3894. (Pubitemid 351484024)
-
(2008)
Bioorganic and Medicinal Chemistry
, vol.16
, Issue.7
, pp. 3887-3894
-
-
Wang, Y.-P.1
Chen, F.-E.2
De Clercq, E.3
Balzarini, J.4
Pannecouque, C.5
-
35
-
-
8744243260
-
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1
-
DOI 10.1021/jm040071z
-
Hopkins, A. L.; Ren, J. S.; Milton, J.; Hazen, R. J.; Chan, J. H.; Stuart, D. I.; Stammers, D. K. Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties.1. J. Med. Chem., 2004, 47, 5912-5922. (Pubitemid 39517015)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.24
, pp. 5912-5922
-
-
Hopkins, A.L.1
Ren, J.2
Milton, J.3
Hazen, R.J.4
Chan, J.H.5
Stuart, D.I.6
Stammers, D.K.7
-
36
-
-
49449113636
-
5-Alkyl-6- benzyl- 2-(2- oxo- 2-phenylethylsulfanyl) pyrimidin- 4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy- benzyloxopyrimidine family with peculiar structure-activity relationship profile
-
Nawrozkij, M. B.; Rotili, D.; Tarantino, D.; Botta, G.; Eremiychuk, A. S.; Musmuca, I.; Ragno, R.; Samuele, A.; Zanoli, S.; Armand-Ugón, M.; Clotet- Codina, I.; Novakov, I. A.; Orlinson, B. S.; Maga, G.; Esté, J. A.; Artico, M.; Mai, A.; 5-Alkyl-6- benzyl- 2-(2- oxo- 2-phenylethylsulfanyl) pyrimidin- 4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy- benzyloxopyrimidine family with peculiar structure-activity relationship profile. J. Med. Chem., 2008, 51, 4641-4652.
-
(2008)
J. Med. Chem.
, vol.51
, pp. 4641-4652
-
-
Nawrozkij, M.B.1
Rotili, D.2
Tarantino, D.3
Botta, G.4
Eremiychuk, A.S.5
Musmuca, I.6
Ragno, R.7
Samuele, A.8
Zanoli, S.9
Armand-Ugón, M.10
Clotet- Codina, I.11
Novakov, I.A.12
Orlinson, B.S.13
Maga, G.14
Esté, J.A.15
Artico, M.16
Mai, A.17
-
37
-
-
71749121628
-
Synthesis and biological evaluation of novel 2-(substituted phenylaminocarbonylmethylthio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)- ones as potent HIV-1 NNRTIs
-
Yu, M.; Liu, X.; Li, Z.; Liu, S.; Pannecouque, C.; De Clercq, E. Synthesis and biological evaluation of novel 2-(substituted phenylaminocarbonylmethylthio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)- ones as potent HIV-1 NNRTIs. Bioorg. Med. Chem., 2009, 17, 7749-7754.
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 7749-7754
-
-
Yu, M.1
Liu, X.2
Li, Z.3
Liu, S.4
Pannecouque, C.5
De Clercq, E.6
-
38
-
-
79954987862
-
Synthesis and biological evaluation of 6-substituted 5-alkyl-2- (phenylaminocarbonylmethylthio) pyrimidin-4(3h)-ones as potent hiv-1 nnrtis
-
Epub ahead of print
-
Yu, M.; Li, Z.; Liu, S.; Fan, E.; Pannecouque, C.; De Clercq, E.; Liu, X. Synthesis and Biological Evaluation of 6-Substituted 5-Alkyl-2- (phenylaminocarbonylmethylthio) pyrimidin-4(3H)-ones as Potent HIV-1 NNRTIs. Chem. Med.Chem., 2011, Epub ahead of print.
-
(2011)
Chem. Med.Chem.
-
-
Yu, M.1
Li, Z.2
Liu, S.3
Fan, E.4
Pannecouque, C.5
De Clercq, E.6
Liu, X.7
-
39
-
-
77951206884
-
Synthesis and biological evaluation of novel C5 halogenfunctionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
-
Qin, H.; Liu, C.; Guo, Y.; Wang, Y.; Zhang, J.; Ma, L.; Zhang, Z.; Wang, X.; Cui, Y.; Liu J. Synthesis and biological evaluation of novel C5 halogenfunctionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorg. Med. Chem,. 2010, 18(9), 3231-3237.
-
(2010)
Bioorg. Med. Chem,.
, vol.18
, Issue.9
, pp. 3231-3237
-
-
Qin, H.1
Liu, C.2
Guo, Y.3
Wang, Y.4
Zhang, J.5
Ma, L.6
Zhang, Z.7
Wang, X.8
Cui, Y.9
Liu, J.10
-
40
-
-
34247268630
-
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6- (arylcarbonyl or α-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
-
DOI 10.1021/jm061167r
-
Ji, L.; Chen, F. E.; De Clercq, E.; Balzarini, J.; Pannecouque, C. Synthesis and Anti-HIV-1 Activity Evaluation of 5-Alkyl-2-alkylthio-6- (arylcarbonyl or α-cyanoarylmethyl)-3,4-dihydropyrimidin- 4(3H)-ones as Novel Nonnucleoside HIV-1 Reverse Transcriptase Inhibitors. J. Med. Chem., 2007, 50, 1778-1786. (Pubitemid 46626589)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.8
, pp. 1778-1786
-
-
Ji, L.1
Chen, F.-E.2
De Clercq, E.3
Balzarini, J.4
Pannecouque, C.5
-
41
-
-
47249122173
-
A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs
-
Radi, M.; Falciani, C.; Contemori, L.; Petricci, E.; Maga, G.; Samuele, A.; Zanoli, S.; Terrazas, M.; Castria, M.; Togninelli, A.; Esté, J. A.; Clotet- Codina, I.; Armand- Ugón, M.; Botta, M. A multidisciplinary approach for the identification of novel HIV-1 non-nucleoside reverse transcriptase inhibitors: S-DABOCs and DAVPs. Chem. Med. Chem., 2008, 3(4), 573-593.
-
(2008)
Chem. Med. Chem.
, vol.3
, Issue.4
, pp. 573-593
-
-
Radi, M.1
Falciani, C.2
Contemori, L.3
Petricci, E.4
Maga, G.5
Samuele, A.6
Zanoli, S.7
Terrazas, M.8
Castria, M.9
Togninelli, A.10
Esté, J.A.11
Clotet- Codina, I.12
Armand-Ugón, M.13
Botta, M.14
-
42
-
-
53949089826
-
Towards novel S-DABOC inhibitors: Synthesis, biological investigation, and molecular modeling studies
-
Radi, M.; Angeli, L.; Franchi, L.; Contemori, L.; Maga, G.; Samuele, A.; Zanoli, S.; Armand-Ugon, M.; Gonzalez, E.; Llano, A.; Esté, J. A.; Botta, M. Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. Bioorg. Med. Chem. Lett., 2008, 18(21), 5777-5780.
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, Issue.21
, pp. 5777-5780
-
-
Radi, M.1
Angeli, L.2
Franchi, L.3
Contemori, L.4
Maga, G.5
Samuele, A.6
Zanoli, S.7
Armand-Ugon, M.8
Gonzalez, E.9
Llano, A.10
Esté, J.A.11
Botta, M.12
-
43
-
-
77950861081
-
Synthesis and biological evaluation of novel 2-arylalkylthio-4- amino-6- benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
-
Qin, H.; Liu, C.; Zhang, J.; Guo, Y.; Zhang, S.; Zhang, Z.; Wang, X.; Zhang, L.; Liu, J. Synthesis and biological evaluation of novel 2-arylalkylthio-4- amino-6- benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors. Bioorg. Med. Chem. Lett., 2010, 20(9), 3003-3005.
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, Issue.9
, pp. 3003-3005
-
-
Qin, H.1
Liu, C.2
Zhang, J.3
Guo, Y.4
Zhang, S.5
Zhang, Z.6
Wang, X.7
Zhang, L.8
Liu, J.9
-
44
-
-
0034256093
-
Designing chiral libraries for drug discovery
-
DOI 10.1016/S1359-6446(00)01515-4, PII S1359644600015154
-
Beroza, P.; Suto, M. J. Designing chiral libraries for drug discovery. Drug Discov. Today, 2000, 5, 364-372. (Pubitemid 30453867)
-
(2000)
Drug Discovery Today
, vol.5
, Issue.8
, pp. 364-372
-
-
Beroza, P.1
Suto, M.J.2
-
45
-
-
0035146092
-
Chiral resolution and molecular modeling investigation of rac-2-cyclopentylthio-6-[1-(2,6- difluorophenyl)ethyl]-3,4-dihydro-5- methylpyrimidin-4(3H)-one (MC- 1047), a potent anti-HIV-1 reverse transcriptase agent of the DABO class
-
Quaglia, M. G.; Mai, A.; Sbardella, G.; Artico, M.; Ragno, R.; Massa, S.; Del Piano, D.; Setzu, G.; Dorattiotto, S.; Cotichini, V. Chiral resolution and molecular modeling investigation of rac-2-cyclopentylthio-6-[1-(2,6- difluorophenyl)ethyl]-3,4-dihydro-5-methylpyrimidin-4(3H)-one (MC- 1047), a potent anti-HIV-1 reverse transcriptase agent of the DABO class. Chirality, 2001, 13, 75-80.
-
(2001)
Chirality
, vol.13
, pp. 75-80
-
-
Quaglia, M.G.1
Mai, A.2
Sbardella, G.3
Artico, M.4
Ragno, R.5
Massa, S.6
Del Piano, D.7
Setzu, G.8
Dorattiotto, S.9
Cotichini, V.10
-
46
-
-
67649403720
-
Chiral hplc separation and absolute configuration of novel s-dabo derivatives
-
Cirilli, R.; Ferretti, R.; La Torre, F.; Borioni, A.; Fares, V.; Camalli, M.; Faggi, C.; Rotili, D.; Mai, A. Chiral HPLC Separation and Absolute Configuration of Novel S-DABO Derivatives. Chirality, 2009, 21, 604-612.
-
(2009)
Chirality
, vol.21
, pp. 604-612
-
-
Cirilli, R.1
Ferretti, R.2
La Torre, F.3
Borioni, A.4
Fares, V.5
Camalli, M.6
Faggi, C.7
Rotili, D.8
Mai, A.9
-
47
-
-
61449115978
-
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyloxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants
-
Radi, M.; Maga, G.; Alongi, M.; Angeli, L.; Samuele, A.; Zanoli, S.; Bellucci, L.; Tafi, A.; Casaluce, G.; Giorgi, G.; Armand-Ugon, M.; Gonzalez, E.; Esté, J. A.; Baltzinger, M.; Bec, G.; Dumas, P.; Ennifar, E.; Botta, M. Discovery of chiral cyclopropyl dihydro-alkylthio-benzyloxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. J. Med. Chem., 2009, 52, 840-851.
-
(2009)
J. Med. Chem.
, vol.52
, pp. 840-851
-
-
Radi, M.1
Maga, G.2
Alongi, M.3
Angeli, L.4
Samuele, A.5
Zanoli, S.6
Bellucci, L.7
Tafi, A.8
Casaluce, G.9
Giorgi, G.10
Armand-Ugon, M.11
Gonzalez, E.12
Esté, J.A.13
Baltzinger, M.14
Bec, G.15
Dumas, P.16
Ennifar, E.17
Botta, M.18
-
48
-
-
37349004798
-
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: Synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants
-
DOI 10.1021/jm0708230
-
Mugnaini, C.; Alongi, M.; Togninelli, A.; Gevariya, H.; Brizzi, A.; Manetti, F.; Bernardini, C.; Angeli, L.; Tafi, A.; Bellucci, L.; Corelli, F.; Massa, S.; Maga, G.; Samuele, A.; Facchini, M.; Clotet-Codina, I.; Armand-Ugón, M.; Esté, J. A.; Botta M. Dihydro-alkylthio-benzyl- oxopyrimidines as Inhibitors of Reverse Transcriptase: Synthesis and Rationalization of the Biological Data on Both Wild-Type Enzyme and Relevant Clinical Mutants. J. Med. Chem., 2007, 50, 6580-6595. (Pubitemid 350309097)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.26
, pp. 6580-6595
-
-
Mugnaini, C.1
Alongi, M.2
Togninelli, A.3
Gevariya, H.4
Brizzi, A.5
Manetti, F.6
Bernardini, C.7
Angeli, L.8
Tafi, A.9
Bellucci, L.10
Corelli, F.11
Massa, S.12
Maga, G.13
Samuele, A.14
Facchini, M.15
Clotet-Codina, I.16
Armand-Ugon, M.17
Este, J.A.18
Botta, M.19
-
49
-
-
35848949355
-
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains
-
DOI 10.1021/jm070811e
-
Mai, A.; Artico, M.; Rotili, D.; Tarantino, D.; Clotet-Codina, I.; Armand- Ugón, M.; Ragno, R.; Simeoni, S.; Sbardella, G.; Nawrozkij, M. B.; Samuele, A.; Maga, G.; Esté, J. A. Synthesis and Biological Properties of Novel 2-Aminopyrimidin-4(3H)-ones Highly Potent against HIV-1 Mutant Strains. J. Med. Chem., 2007, 50, 5412-5424. (Pubitemid 350057851)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.22
, pp. 5412-5424
-
-
Mai, A.1
Artico, M.2
Rotili, D.3
Tarantino, D.4
Clotet-Codina, I.5
Armand-Ugon, M.6
Ragno, R.7
Simeoni, S.8
Sbardella, G.9
Nawrozkij, M.B.10
Samuele, A.11
Maga, G.12
Este, J.A.13
-
50
-
-
12144278681
-
HIV-reverse transcriptase inhibition: Inclusion of ligand-induced fit by cross-docking studies
-
DOI 10.1021/jm0493921
-
Ragno, R.; Frasca, S.; Manetti, F.; Brizzi, A.; Massa, S. HIV-Reverse Transcriptase Inhibition: Inclusion of Ligand-Induced Fit by Cross-Docking Studies. J. Med. Chem., 2005, 48, 200-212. (Pubitemid 40109511)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.1
, pp. 200-212
-
-
Ragno, R.1
Frasca, S.2
Manetti, F.3
Brizzi, A.4
Massa, S.5
-
51
-
-
52049088542
-
3D-QSAR CoMFA of a series of DABO derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors
-
de Brito, M. A.; Rodrigues, C. R.; Cirino, J. J.; de Alencastro, R. B.; Castro, H. C.; Albuquerque, M.G. 3D-QSAR CoMFA of a series of DABO derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors. J. Chem. Inf. Model., 2008, 48, 1706-1715.
-
(2008)
J. Chem. Inf. Model.
, vol.48
, pp. 1706-1715
-
-
De Brito, M.A.1
Rodrigues, C.R.2
Cirino, J.J.3
De Alencastro, R.B.4
Castro, H.C.5
Albuquerque, M.G.6
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