-
1
-
-
84874114410
-
Antivirals: Past, present and future
-
E. De Clercq Antivirals: past, present and future Biochem. Pharmacol. 2013 85 727 744
-
(2013)
Biochem. Pharmacol.
, vol.85
, pp. 727-744
-
-
De Clercq, E.1
-
2
-
-
84867403312
-
Human viral diseases: What is next for antiviral drug discovery?
-
E. De Clercq Human viral diseases: what is next for antiviral drug discovery? Curr. Opin. Virol. 2012 2 572 579
-
(2012)
Curr. Opin. Virol.
, vol.2
, pp. 572-579
-
-
De Clercq, E.1
-
3
-
-
84870202766
-
New therapeutic landscape of NNRTIs for treatment of HIV: A look at recent data
-
D. Jayaweera P. Dilanchian New therapeutic landscape of NNRTIs for treatment of HIV: a look at recent data Expert Opin. Pharmacother. 2012 13 2601 2612
-
(2012)
Expert Opin. Pharmacother.
, vol.13
, pp. 2601-2612
-
-
Jayaweera, D.1
Dilanchian, P.2
-
4
-
-
70349395798
-
Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update
-
P. Zhan X. Liu Z. Li Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006-2008 update Curr. Med. Chem. 2009 16 2876 2889
-
(2009)
Curr. Med. Chem.
, vol.16
, pp. 2876-2889
-
-
Zhan, P.1
Liu, X.2
Li, Z.3
-
6
-
-
84876852661
-
Structural diversity, pharmacophore similarity, and implications for drug design
-
10.1002/med.20241
-
P. Zhan X. Chen D. Li Z. Fang E. De Clercq X. Liu Structural diversity, pharmacophore similarity, and implications for drug design Med. Res. Rev. 2011 10.1002/med.20241
-
(2011)
Med. Res. Rev.
-
-
Zhan, P.1
Chen, X.2
Li, D.3
Fang, Z.4
De Clercq, E.5
Liu, X.6
-
7
-
-
79955104761
-
Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: A patent review (2005-2010)
-
P. Zhan X. Liu Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2005-2010) Expert Opin. Ther. Pat. 2011 5 717 796
-
(2011)
Expert Opin. Ther. Pat.
, vol.5
, pp. 717-796
-
-
Zhan, P.1
Liu, X.2
-
8
-
-
68149109726
-
Sulfanyltriazole/tetrazoles: A promising class of HIV-1 NNRTIs
-
P. Zhan Z. Li X. Liu E. De Clercq Sulfanyltriazole/tetrazoles: a promising class of HIV-1 NNRTIs Mini-Rev. Med. Chem. 2009 9 1014 1023
-
(2009)
Mini-Rev. Med. Chem.
, vol.9
, pp. 1014-1023
-
-
Zhan, P.1
Li, Z.2
Liu, X.3
De Clercq, E.4
-
9
-
-
33745727133
-
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors
-
Z. Wang B. Wu K. L. Kuhen B. Bursulaya T. N. Nguyen D. G. Nguyen Y. He Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors Bioorg. Med. Chem. Lett. 2006 16 4174 4177
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4174-4177
-
-
Wang, Z.1
Wu, B.2
Kuhen, K.L.3
Bursulaya, B.4
Nguyen, T.N.5
Nguyen, D.G.6
He, Y.7
-
10
-
-
33746233238
-
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase
-
M. De La Rosa H. W. Kim E. Gunic C. Jenket U. Boyle Y. H. Koh I. Korboukh M. Allan W. Zhang H. Chen W. Xu S. Nilar N. Yao R. Hamatake S. A. Lang Z. Hong Z. Zhang J. L. Girardet Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase Bioorg. Med. Chem. Lett. 2006 16 4444 4449
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4444-4449
-
-
De La Rosa, M.1
Kim, H.W.2
Gunic, E.3
Jenket, C.4
Boyle, U.5
Koh, Y.H.6
Korboukh, I.7
Allan, M.8
Zhang, W.9
Chen, H.10
Xu, W.11
Nilar, S.12
Yao, N.13
Hamatake, R.14
Lang, S.A.15
Hong, Z.16
Zhang, Z.17
Girardet, J.L.18
-
11
-
-
33645886644
-
Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant
-
E. Muraglia O. D. Kinzel R. Laufer M. D. Miller G. Moyer V. Munshi F. Orvieto M. C. Palumbi G. Pescatore M. Rowley P. D. Williams V. Summa Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant Bioorg. Med. Chem. Lett. 2006 16 2748 2752
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 2748-2752
-
-
Muraglia, E.1
Kinzel, O.D.2
Laufer, R.3
Miller, M.D.4
Moyer, G.5
Munshi, V.6
Orvieto, F.7
Palumbi, M.C.8
Pescatore, G.9
Rowley, M.10
Williams, P.D.11
Summa, V.12
-
12
-
-
34249327726
-
Scaffold hopping in the rational design of novel HIV-1 non-nucleoside reverse transcriptase inhibitors
-
J. A. O'Meara A. Jakalian S. LaPlante P. R. Bonneau R. Coulombe A. M. Faucher I. Guse S. Landry J. Racine B. Simoneau B. Thavonekham C. Yoakim Scaffold hopping in the rational design of novel HIV-1 non-nucleoside reverse transcriptase inhibitors Bioorg. Med. Chem. Lett. 2007 17 3362 3366
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 3362-3366
-
-
O'Meara, J.A.1
Jakalian, A.2
Laplante, S.3
Bonneau, P.R.4
Coulombe, R.5
Faucher, A.M.6
Guse, I.7
Landry, S.8
Racine, J.9
Simoneau, B.10
Thavonekham, B.11
Yoakim, C.12
-
13
-
-
34447319100
-
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases
-
A. Gagnon M. H. Amad P. R. Bonneau R. Coulombe P. L. DeRoy L. Doyon J. Duan M. Garneau I. Guse A. Jakalian E. Jolicoeur S. Landry E. Malenfant B. Simoneau C. Yoakim Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases Bioorg. Med. Chem. Lett. 2007 17 4437 4441
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 4437-4441
-
-
Gagnon, A.1
Amad, M.H.2
Bonneau, P.R.3
Coulombe, R.4
Deroy, P.L.5
Doyon, L.6
Duan, J.7
Garneau, M.8
Guse, I.9
Jakalian, A.10
Jolicoeur, E.11
Landry, S.12
Malenfant, E.13
Simoneau, B.14
Yoakim, C.15
-
14
-
-
59649115687
-
Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases
-
A. Gagnon S. Landry R. Coulombe A. Jakalian I. Guse B. Thavonekham P. R. Bonneau C. Yoakim B. Simoneau Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases Bioorg. Med. Chem. Lett. 2009 19 1199 1205
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 1199-1205
-
-
Gagnon, A.1
Landry, S.2
Coulombe, R.3
Jakalian, A.4
Guse, I.5
Thavonekham, B.6
Bonneau, P.R.7
Yoakim, C.8
Simoneau, B.9
-
15
-
-
77955386895
-
Phase 2a randomized controlled trial of short-term activity, safety, and pharmacokinetics of a novel non-nucleoside reverse transcriptase inhibitor, RDEA806, in HIV-1-positive, antiretroviral-naive subjects
-
G. Moyle M. Boffito A. Stoehr A. Rieger Z. Shen K. Manhard B. Sheedy V. Hingorani A. Raney M. Nguyen T. Nguyen V. Ong L. T. Yeh B. Quart Phase 2a randomized controlled trial of short-term activity, safety, and pharmacokinetics of a novel non-nucleoside reverse transcriptase inhibitor, RDEA806, in HIV-1-positive, antiretroviral-naive subjects Antimicrob. Agents Chemother. 2010 54 3170 3178
-
(2010)
Antimicrob. Agents Chemother.
, vol.54
, pp. 3170-3178
-
-
Moyle, G.1
Boffito, M.2
Stoehr, A.3
Rieger, A.4
Shen, Z.5
Manhard, K.6
Sheedy, B.7
Hingorani, V.8
Raney, A.9
Nguyen, M.10
Nguyen, T.11
Ong, V.12
Yeh, L.T.13
Quart, B.14
-
16
-
-
84860289205
-
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: Lessons from the development of seven representative paradigms
-
D. Li P. Zhan E. De Clercq X. Liu Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms J. Med. Chem. 2012 55 3595 3613
-
(2012)
J. Med. Chem.
, vol.55
, pp. 3595-3613
-
-
Li, D.1
Zhan, P.2
De Clercq, E.3
Liu, X.4
-
17
-
-
53349162138
-
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors
-
P. Zhan X. Liu Y. Cao Y. Wang C. Pannecouque E. De Clercq 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors Bioorg. Med. Chem. Lett. 2008 18 5368 5371
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 5368-5371
-
-
Zhan, P.1
Liu, X.2
Cao, Y.3
Wang, Y.4
Pannecouque, C.5
De Clercq, E.6
-
18
-
-
68149145657
-
Novel 1,2,3-thiadiazole derivatives as HIV-1 NNRTIs with improved potency: Synthesis and preliminary SAR studies
-
P. Zhan X. Liu Z. Li Z. Fang Z. Li D. Wang C. Pannecouque E. De Clercq Novel 1,2,3-thiadiazole derivatives as HIV-1 NNRTIs with improved potency: synthesis and preliminary SAR studies Bioorg. Med. Chem. 2009 17 5920 5927
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 5920-5927
-
-
Zhan, P.1
Liu, X.2
Li, Z.3
Fang, Z.4
Li, Z.5
Wang, D.6
Pannecouque, C.7
De Clercq, E.8
-
19
-
-
70349774254
-
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2, 3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
-
P. Zhan X. Liu Z. Fang Z. Li C. Pannecouque E. De Clercq Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5- ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors Eur. J. Med. Chem. 2009 44 4648 4653
-
(2009)
Eur. J. Med. Chem.
, vol.44
, pp. 4648-4653
-
-
Zhan, P.1
Liu, X.2
Fang, Z.3
Li, Z.4
Pannecouque, C.5
De Clercq, E.6
-
20
-
-
77954695191
-
1,2,3-Thiadiazole thioacetanilides. Part 2: Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl] sulfanyl}acetanilides as HIV-1 inhibitors
-
P. Zhan X. Liu Z. Li Z. Fang C. Pannecouque E. De Clercq 1,2,3-Thiadiazole thioacetanilides. Part 2: synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl} acetanilides as HIV-1 inhibitors Chem. Biodiversity 2010 7 1717 1727
-
(2010)
Chem. Biodiversity
, vol.7
, pp. 1717-1727
-
-
Zhan, P.1
Liu, X.2
Li, Z.3
Fang, Z.4
Pannecouque, C.5
De Clercq, E.6
-
21
-
-
68149089670
-
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
-
P. Zhan X. Liu J. Zhu Z. Fang Z. Li C. Pannecouque E. De Clercq Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors Bioorg. Med. Chem. 2009 17 5775 5781
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 5775-5781
-
-
Zhan, P.1
Liu, X.2
Zhu, J.3
Fang, Z.4
Li, Z.5
Pannecouque, C.6
De Clercq, E.7
-
22
-
-
68649109125
-
1,2,3-Selenadiazole thioacetanilides: Synthesis and anti-HIV activity evaluation
-
P. Zhan X. Liu Z. Fang C. Pannecouque E. De Clercq 1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation Bioorg. Med. Chem. 2009 17 6374 6379
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 6374-6379
-
-
Zhan, P.1
Liu, X.2
Fang, Z.3
Pannecouque, C.4
De Clercq, E.5
-
23
-
-
77956478098
-
Synthesis and anti-HIV activity evaluation of novel N′-arylidene-2- [1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio] acetohy drazides
-
P. Zhan H. Liu X. Liu Y. Wang C. Pannecouque M. Witvrouw E. De Clercq Synthesis and anti-HIV activity evaluation of novel N′-arylidene-2-[1- (naphthalen-1-yl)-1H-tetrazol-5-ylthio] acetohy drazides Med. Chem. Res. 2009 19 652 663
-
(2009)
Med. Chem. Res.
, vol.19
, pp. 652-663
-
-
Zhan, P.1
Liu, H.2
Liu, X.3
Wang, Y.4
Pannecouque, C.5
Witvrouw, M.6
De Clercq, E.7
-
24
-
-
80053197763
-
Arylazolylthioacetanilide. Part 8*: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3- ylthio)-N-arylacetamides as potent HIV-1 inhibitors
-
P. Zhan X. Chen X. Li D. Li Y. Tian W. Chen C. Pannecouque E. De Clercq X. Liu Arylazolylthioacetanilide. Part 8*: design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3- ylthio)-N-arylacetamides as potent HIV-1 inhibitors Eur. J. Med. Chem. 2011 46 5039 5045
-
(2011)
Eur. J. Med. Chem.
, vol.46
, pp. 5039-5045
-
-
Zhan, P.1
Chen, X.2
Li, X.3
Li, D.4
Tian, Y.5
Chen, W.6
Pannecouque, C.7
De Clercq, E.8
Liu, X.9
-
25
-
-
84864940620
-
Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and biological investigation of thiazolylthioacetamides derivatives as a novel class of potential antiviral agents
-
P. Zhan L. Wang H. Liu X. Chen X. Li X. Jiang Q. Zhang X. Liu C. Pannecouque L. Naesens E. De Clercq A. Liu G. Du Arylazolyl(azinyl) thioacetanilide. Part 9: synthesis and biological investigation of thiazolylthioacetamides derivatives as a novel class of potential antiviral agents Arch. Pharmacal Res. 2012 35 975 986
-
(2012)
Arch. Pharmacal Res.
, vol.35
, pp. 975-986
-
-
Zhan, P.1
Wang, L.2
Liu, H.3
Chen, X.4
Li, X.5
Jiang, X.6
Zhang, Q.7
Liu, X.8
Pannecouque, C.9
Naesens, L.10
De Clercq, E.11
Liu, A.12
Du, G.13
-
26
-
-
7744243992
-
Bioisosterism: A rational approach in drug design
-
G. A. Patani E. J. LaVoie Bioisosterism: a rational approach in drug design Chem. Rev. 1996 96 3147 3176
-
(1996)
Chem. Rev.
, vol.96
, pp. 3147-3176
-
-
Patani, G.A.1
Lavoie, E.J.2
-
27
-
-
0034924558
-
The use of bioisosteric groups in lead optimization
-
P. H. Olesen The use of bioisosteric groups in lead optimization Curr. Opin. Drug Discovery Dev. 2001 4 471 478
-
(2001)
Curr. Opin. Drug Discovery Dev.
, vol.4
, pp. 471-478
-
-
Olesen, P.H.1
-
28
-
-
11844255399
-
Bioisosterism: A useful strategy for molecular modification and drug design
-
L. M. Lima E. J. Barreiro Bioisosterism: a useful strategy for molecular modification and drug design Curr. Med. Chem. 2005 12 23 49
-
(2005)
Curr. Med. Chem.
, vol.12
, pp. 23-49
-
-
Lima, L.M.1
Barreiro, E.J.2
-
29
-
-
67349142564
-
Medicinal chemistry strategies in follow-on drug discovery
-
H. Zhao Z. Guo Medicinal chemistry strategies in follow-on drug discovery Drug Discovery Today 2009 14 516 522
-
(2009)
Drug Discovery Today
, vol.14
, pp. 516-522
-
-
Zhao, H.1
Guo, Z.2
-
31
-
-
33847664739
-
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro) -5′-N-ethylcarboxamido-adenosines: The first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor
-
P. G. Baraldi D. Preti M. A. Tabrizi F. Fruttarolo G. Saponaro S. Baraldi R. Romagnoli A. R. Moorman S. Gessi K. Varani P. A. Borea N(6)-[(hetero)aryl/ (cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5′-N-ethylcarboxamido- adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor Bioorg. Med. Chem. 2007 15 2514 2527
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 2514-2527
-
-
Baraldi, P.G.1
Preti, D.2
Tabrizi, M.A.3
Fruttarolo, F.4
Saponaro, G.5
Baraldi, S.6
Romagnoli, R.7
Moorman, A.R.8
Gessi, S.9
Varani, K.10
Borea, P.A.11
-
33
-
-
0021237243
-
Detection, isolation, and continuous production of cytopathic retroviruses (HTLV-III) from patients with AIDS and pre-AIDS
-
M. Popovic M. G. Sarngadharan E. Read R. C. Gallo Detection, isolation, and continuous production of cytopathic retroviruses (HTLV-III) from patients with AIDS and pre-AIDS Science 1984 224 497 500
-
(1984)
Science
, vol.224
, pp. 497-500
-
-
Popovic, M.1
Sarngadharan, M.G.2
Read, E.3
Gallo, R.C.4
-
34
-
-
0020596551
-
Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS)
-
F. Barré-Sinoussi J. C. Chermann F. Rey M. T. Nugeyre S. Chamaret J. Gruest C. Dauguet C. Axler-Blin F. Vézinet-Brun C. Rouzioux W. Rozenbaum L. Montagnier Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS) Science 1983 220 868 871
-
(1983)
Science
, vol.220
, pp. 868-871
-
-
Barré-Sinoussi, F.1
Chermann, J.C.2
Rey, F.3
Nugeyre, M.T.4
Chamaret, S.5
Gruest, J.6
Dauguet, C.7
Axler-Blin, C.8
Vézinet-Brun, F.9
Rouzioux, C.10
Rozenbaum, W.11
Montagnier, L.12
-
35
-
-
0023687234
-
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds
-
R. Pauwels J. Balzarini M. Baba R. Snoeck D. Schols P. Herdewijn J. Desmyter E. De Clercq Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds J. Virol. Methods 1988 20 309 321
-
(1988)
J. Virol. Methods
, vol.20
, pp. 309-321
-
-
Pauwels, R.1
Balzarini, J.2
Baba, M.3
Snoeck, R.4
Schols, D.5
Herdewijn, P.6
Desmyter, J.7
De Clercq, E.8
-
36
-
-
40749129190
-
Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: Revisited 20 years later
-
C. Pannecouque D. Daelemans E. De Clercq Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later Nat. Protocols 2008 3 427 434
-
(2008)
Nat. Protocols
, vol.3
, pp. 427-434
-
-
Pannecouque, C.1
Daelemans, D.2
De Clercq, E.3
-
38
-
-
34548388846
-
Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4- triazole as potential HIV-1 NNRTIs
-
J. Wu X. Liu X. Cheng Y. Cao D. Wang Z. Li W. Xu C. Pannecouque M. Witvrouw E. De Clercq Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5- mercapto-1,2,4-triazole as potential HIV-1 NNRTIs. Molecules 2007 12 2003 2016
-
(2007)
Molecules
, vol.12
, pp. 2003-2016
-
-
Wu, J.1
Liu, X.2
Cheng, X.3
Cao, Y.4
Wang, D.5
Li, Z.6
Xu, W.7
Pannecouque, C.8
Witvrouw, M.9
De Clercq, E.10
|