-
1
-
-
84962566015
-
Tuberculosis – advances in development of new drugs, treatment regimens, host-directed therapies, and biomarkers
-
1 Wallis, R.S., et al. Tuberculosis – advances in development of new drugs, treatment regimens, host-directed therapies, and biomarkers. Lancet Infect. Dis. 16 (2016), e34–e46.
-
(2016)
Lancet Infect. Dis.
, vol.16
, pp. e34-e46
-
-
Wallis, R.S.1
-
2
-
-
79251589638
-
The challenge of new drug discovery for tuberculosis
-
2 Koul, A., et al. The challenge of new drug discovery for tuberculosis. Nature 469 (2011), 483–490.
-
(2011)
Nature
, vol.469
, pp. 483-490
-
-
Koul, A.1
-
3
-
-
33845903833
-
Drugs for bad bugs: confronting the challenges of antibacterial discovery
-
3 Payne, D.J., et al. Drugs for bad bugs: confronting the challenges of antibacterial discovery. Nat. Rev. Drug Discov. 6 (2007), 29–40.
-
(2007)
Nat. Rev. Drug Discov.
, vol.6
, pp. 29-40
-
-
Payne, D.J.1
-
4
-
-
84877267006
-
Advances in the development of new tuberculosis drugs and treatment regimens
-
4 Zumla, A., et al. Advances in the development of new tuberculosis drugs and treatment regimens. Nat. Rev. Drug Discov. 12 (2013), 388–404.
-
(2013)
Nat. Rev. Drug Discov.
, vol.12
, pp. 388-404
-
-
Zumla, A.1
-
5
-
-
84943664518
-
The association between sterilizing activity and drug distribution into tuberculosis lesions
-
5 Prideaux, B., et al. The association between sterilizing activity and drug distribution into tuberculosis lesions. Nat. Med. 21 (2015), 1223–1227.
-
(2015)
Nat. Med.
, vol.21
, pp. 1223-1227
-
-
Prideaux, B.1
-
6
-
-
0036051992
-
High-throughput crystallography for lead discovery in drug design
-
6 Blundell, T.L., et al. High-throughput crystallography for lead discovery in drug design. Nat. Rev. Drug Discov. 1 (2002), 45–54.
-
(2002)
Nat. Rev. Drug Discov.
, vol.1
, pp. 45-54
-
-
Blundell, T.L.1
-
7
-
-
84887001050
-
A three-stage biophysical screening cascade for fragment-based drug discovery
-
7 Mashalidis, E.H., et al. A three-stage biophysical screening cascade for fragment-based drug discovery. Nat. Protoc. 8 (2013), 2309–2324.
-
(2013)
Nat. Protoc.
, vol.8
, pp. 2309-2324
-
-
Mashalidis, E.H.1
-
8
-
-
84978474564
-
Twenty years on: the impact of fragments on drug discovery
-
8 Erlanson, D.A., et al. Twenty years on: the impact of fragments on drug discovery. Nat. Rev. Drug Discov. 15 (2016), 605–619.
-
(2016)
Nat. Rev. Drug Discov.
, vol.15
, pp. 605-619
-
-
Erlanson, D.A.1
-
9
-
-
84862869077
-
Fragment-based approaches in drug discovery and chemical biology
-
9 Scott, D.E., et al. Fragment-based approaches in drug discovery and chemical biology. Biochemistry 51 (2012), 4990–5003.
-
(2012)
Biochemistry
, vol.51
, pp. 4990-5003
-
-
Scott, D.E.1
-
10
-
-
67849113794
-
The rise of fragment-based drug discovery
-
10 Murray, C.W., Rees, D.C., The rise of fragment-based drug discovery. Nat. Chem. 1 (2009), 187–192.
-
(2009)
Nat. Chem.
, vol.1
, pp. 187-192
-
-
Murray, C.W.1
Rees, D.C.2
-
11
-
-
37249005205
-
The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability
-
11 Niesen, F.H., et al. The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability. Nat. Protoc. 2 (2007), 2212–2221.
-
(2007)
Nat. Protoc.
, vol.2
, pp. 2212-2221
-
-
Niesen, F.H.1
-
12
-
-
84908342421
-
Determination of protein–ligand interactions using differential scanning fluorimetry
-
12 Vivoli, M., et al. Determination of protein–ligand interactions using differential scanning fluorimetry. J. Vis. Exp., 91, 2014, 51809.
-
(2014)
J. Vis. Exp.
, vol.91
, pp. 51809
-
-
Vivoli, M.1
-
13
-
-
0035692794
-
WaterLOGSY as a method for primary NMR screening: practical aspects and range of applicability
-
13 Dalvit, C., et al. WaterLOGSY as a method for primary NMR screening: practical aspects and range of applicability. J. Biomol. NMR 21 (2001), 349–359.
-
(2001)
J. Biomol. NMR
, vol.21
, pp. 349-359
-
-
Dalvit, C.1
-
14
-
-
35848961691
-
NMR-based screening: a powerful tool in fragment-based drug discovery
-
14 Klages, J., et al. NMR-based screening: a powerful tool in fragment-based drug discovery. Analyst 132 (2007), 693–705.
-
(2007)
Analyst
, vol.132
, pp. 693-705
-
-
Klages, J.1
-
15
-
-
0033553844
-
Characterization of ligand binding by saturation transfer difference NMR spectroscopy
-
15 Mayer, M., Meyer, B., Characterization of ligand binding by saturation transfer difference NMR spectroscopy. Angew. Chem. Int. Ed. Engl. 38 (1999), 1784–1788.
-
(1999)
Angew. Chem. Int. Ed. Engl.
, vol.38
, pp. 1784-1788
-
-
Mayer, M.1
Meyer, B.2
-
16
-
-
0031576702
-
One-dimensional relaxation- and diffusion-edited NMR methods for screening compounds that bind to macromolecules
-
16 Hajduk, P.J., et al. One-dimensional relaxation- and diffusion-edited NMR methods for screening compounds that bind to macromolecules. J. Am. Chem. Soc. 119 (1997), 12257–12261.
-
(1997)
J. Am. Chem. Soc.
, vol.119
, pp. 12257-12261
-
-
Hajduk, P.J.1
-
17
-
-
77956622674
-
Fragment screening by surface plasmon resonance
-
17 Navratilova, I., Hopkins, A.L., Fragment screening by surface plasmon resonance. ACS Med. Chem. Lett. 1 (2010), 44–48.
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, pp. 44-48
-
-
Navratilova, I.1
Hopkins, A.L.2
-
18
-
-
80051787791
-
Biosensor-based small molecule fragment screening with biolayer interferometry
-
18 Wartchow, C.A., et al. Biosensor-based small molecule fragment screening with biolayer interferometry. J. Comput. Aided Mol. Des. 25 (2011), 669–676.
-
(2011)
J. Comput. Aided Mol. Des.
, vol.25
, pp. 669-676
-
-
Wartchow, C.A.1
-
19
-
-
84856369753
-
Automated protein–ligand interaction screening by mass spectrometry
-
19 Maple, H.J., et al. Automated protein–ligand interaction screening by mass spectrometry. J. Med. Chem. 55 (2012), 837–851.
-
(2012)
J. Med. Chem.
, vol.55
, pp. 837-851
-
-
Maple, H.J.1
-
20
-
-
84961262682
-
An automated microscale thermophoresis screening approach for fragment-based lead discovery
-
20 Linke, P., et al. An automated microscale thermophoresis screening approach for fragment-based lead discovery. J. Biomol. Screen. 21 (2016), 414–421.
-
(2016)
J. Biomol. Screen.
, vol.21
, pp. 414-421
-
-
Linke, P.1
-
21
-
-
84940460179
-
One question, multiple answers: biochemical and biophysical screening methods retrieve deviating fragment hit lists
-
21 Schiebel, J., et al. One question, multiple answers: biochemical and biophysical screening methods retrieve deviating fragment hit lists. ChemMedChem 10 (2015), 1511–1521.
-
(2015)
ChemMedChem
, vol.10
, pp. 1511-1521
-
-
Schiebel, J.1
-
22
-
-
84863209627
-
Antibody-enabled small-molecule drug discovery
-
22 Lawson, A.D., Antibody-enabled small-molecule drug discovery. Nat. Rev. Drug Discov. 11 (2012), 519–525.
-
(2012)
Nat. Rev. Drug Discov.
, vol.11
, pp. 519-525
-
-
Lawson, A.D.1
-
23
-
-
84981532009
-
Biophysics in drug discovery: impact, challenges and opportunities
-
23 Renaud, J.P., et al. Biophysics in drug discovery: impact, challenges and opportunities. Nat. Rev. Drug Discov. 15 (2016), 679–698.
-
(2016)
Nat. Rev. Drug Discov.
, vol.15
, pp. 679-698
-
-
Renaud, J.P.1
-
24
-
-
84946204230
-
Lessons from hot spot analysis for fragment-based drug discovery
-
24 Hall, D.R., et al. Lessons from hot spot analysis for fragment-based drug discovery. Trends Pharmacol. Sci. 36 (2015), 724–736.
-
(2015)
Trends Pharmacol. Sci.
, vol.36
, pp. 724-736
-
-
Hall, D.R.1
-
25
-
-
84969497984
-
Identifying interactions that determine fragment binding at protein hotspots
-
25 Radoux, C.J., et al. Identifying interactions that determine fragment binding at protein hotspots. J. Med. Chem. 59 (2016), 4314–4325.
-
(2016)
J. Med. Chem.
, vol.59
, pp. 4314-4325
-
-
Radoux, C.J.1
-
26
-
-
19544372226
-
Coenzyme A: back in action
-
26 Leonardi, R., et al. Coenzyme A: back in action. Prog. Lipid Res. 44 (2005), 125–153.
-
(2005)
Prog. Lipid Res.
, vol.44
, pp. 125-153
-
-
Leonardi, R.1
-
27
-
-
84881423067
-
Integrated biophysical approach to fragment screening and validation for fragment-based lead discovery
-
27 Silvestre, H.L., et al. Integrated biophysical approach to fragment screening and validation for fragment-based lead discovery. Proc. Natl. Acad. Sci. U. S. A. 110 (2013), 12984–12989.
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 12984-12989
-
-
Silvestre, H.L.1
-
28
-
-
70350346470
-
Application of fragment growing and fragment linking to the discovery of inhibitors of Mycobacterium tuberculosis pantothenate synthetase
-
28 Hung, A.W., et al. Application of fragment growing and fragment linking to the discovery of inhibitors of Mycobacterium tuberculosis pantothenate synthetase. Angew. Chem. Int. Ed. Engl. 48 (2009), 8452–8456.
-
(2009)
Angew. Chem. Int. Ed. Engl.
, vol.48
, pp. 8452-8456
-
-
Hung, A.W.1
-
29
-
-
84954028329
-
Optimization of inhibitors of Mycobacterium tuberculosis pantothenate synthetase based on group efficiency analysis
-
29 Hung, A.W., et al. Optimization of inhibitors of Mycobacterium tuberculosis pantothenate synthetase based on group efficiency analysis. ChemMedChem 11 (2016), 38–42.
-
(2016)
ChemMedChem
, vol.11
, pp. 38-42
-
-
Hung, A.W.1
-
30
-
-
84945264516
-
Assembly of the mycobacterial cell wall
-
30 Jankute, M., et al. Assembly of the mycobacterial cell wall. Annu. Rev. Microbiol. 69 (2015), 405–423.
-
(2015)
Annu. Rev. Microbiol.
, vol.69
, pp. 405-423
-
-
Jankute, M.1
-
31
-
-
0036090968
-
Evidence for a partial redundancy of the fibronectin-binding proteins for the transfer of mycoloyl residues onto the cell wall arabinogalactan termini of Mycobacterium tuberculosis
-
31 Puech, V., et al. Evidence for a partial redundancy of the fibronectin-binding proteins for the transfer of mycoloyl residues onto the cell wall arabinogalactan termini of Mycobacterium tuberculosis. Mol. Microbiol. 44 (2002), 1109–1122.
-
(2002)
Mol. Microbiol.
, vol.44
, pp. 1109-1122
-
-
Puech, V.1
-
32
-
-
0031007903
-
Role of the major antigen of Mycobacterium tuberculosis in cell wall biogenesis
-
32 Belisle, J.T., et al. Role of the major antigen of Mycobacterium tuberculosis in cell wall biogenesis. Science 276 (1997), 1420–1422.
-
(1997)
Science
, vol.276
, pp. 1420-1422
-
-
Belisle, J.T.1
-
33
-
-
0032982736
-
Inactivation of the antigen 85C gene profoundly affects the mycolate content and alters the permeability of the Mycobacterium tuberculosis cell envelope
-
33 Jackson, M., et al. Inactivation of the antigen 85C gene profoundly affects the mycolate content and alters the permeability of the Mycobacterium tuberculosis cell envelope. Mol. Microbiol. 31 (1999), 1573–1587.
-
(1999)
Mol. Microbiol.
, vol.31
, pp. 1573-1587
-
-
Jackson, M.1
-
34
-
-
84889248820
-
Mechanism of inhibition of Mycobacterium tuberculosis antigen 85 by ebselen
-
34 Favrot, L., et al. Mechanism of inhibition of Mycobacterium tuberculosis antigen 85 by ebselen. Nat. Commun., 4, 2013, 2748.
-
(2013)
Nat. Commun.
, vol.4
, pp. 2748
-
-
Favrot, L.1
-
35
-
-
78649858286
-
Novel small molecule inhibitors of MDR Mycobacterium tuberculosis by NMR fragment screening of antigen 85C
-
35 Scheich, C., et al. Novel small molecule inhibitors of MDR Mycobacterium tuberculosis by NMR fragment screening of antigen 85C. J. Med. Chem. 53 (2010), 8362–8367.
-
(2010)
J. Med. Chem.
, vol.53
, pp. 8362-8367
-
-
Scheich, C.1
-
36
-
-
27744492218
-
Conditional depletion of KasA, a key enzyme of mycolic acid biosynthesis, leads to mycobacterial cell lysis
-
36 Bhatt, A., et al. Conditional depletion of KasA, a key enzyme of mycolic acid biosynthesis, leads to mycobacterial cell lysis. J. Bacteriol. 187 (2005), 7596–7606.
-
(2005)
J. Bacteriol.
, vol.187
, pp. 7596-7606
-
-
Bhatt, A.1
-
37
-
-
33744994317
-
Platensimycin is a selective FabF inhibitor with potent antibiotic properties
-
37 Wang, J., et al. Platensimycin is a selective FabF inhibitor with potent antibiotic properties. Nature 441 (2006), 358–361.
-
(2006)
Nature
, vol.441
, pp. 358-361
-
-
Wang, J.1
-
38
-
-
0035794127
-
Inhibition of beta-ketoacyl-acyl carrier protein synthases by thiolactomycin and cerulenin. Structure and mechanism
-
38 Price, A.C., et al. Inhibition of beta-ketoacyl-acyl carrier protein synthases by thiolactomycin and cerulenin. Structure and mechanism. J. Biol. Chem. 276 (2001), 6551–6559.
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 6551-6559
-
-
Price, A.C.1
-
39
-
-
84874775139
-
Thiolactomycin-based beta-ketoacyl-AcpM synthase A (KasA) inhibitors: fragment-based inhibitor discovery using transient one-dimensional nuclear overhauser effect NMR spectroscopy
-
39 Kapilashrami, K., et al. Thiolactomycin-based beta-ketoacyl-AcpM synthase A (KasA) inhibitors: fragment-based inhibitor discovery using transient one-dimensional nuclear overhauser effect NMR spectroscopy. J. Biol. Chem. 288 (2013), 6045–6052.
-
(2013)
J. Biol. Chem.
, vol.288
, pp. 6045-6052
-
-
Kapilashrami, K.1
-
40
-
-
84887928420
-
Isoniazid: an update on the multiple mechanisms for a singular action
-
40 Bernardes-Genisson, V., et al. Isoniazid: an update on the multiple mechanisms for a singular action. Curr. Med. Chem. 20 (2013), 4370–4385.
-
(2013)
Curr. Med. Chem.
, vol.20
, pp. 4370-4385
-
-
Bernardes-Genisson, V.1
-
41
-
-
85007428022
-
Mycobacterium tuberculosis whole genome sequencing and protein structure modelling provides insights into anti-tuberculosis drug resistance
-
41 Phelan, J., et al. Mycobacterium tuberculosis whole genome sequencing and protein structure modelling provides insights into anti-tuberculosis drug resistance. BMC Med., 14, 2016, 31.
-
(2016)
BMC Med.
, vol.14
, pp. 31
-
-
Phelan, J.1
-
42
-
-
84896848906
-
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA
-
42 Encinas, L., et al. Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA. J. Med. Chem. 57 (2014), 1276–1288.
-
(2014)
J. Med. Chem.
, vol.57
, pp. 1276-1288
-
-
Encinas, L.1
-
43
-
-
84920711914
-
Direct inhibitors of InhA are active against Mycobacterium tuberculosis
-
43 Manjunatha, U.H., et al. Direct inhibitors of InhA are active against Mycobacterium tuberculosis. Sci. Transl. Med., 7, 2015, 269ra263.
-
(2015)
Sci. Transl. Med.
, vol.7
, pp. 269ra263
-
-
Manjunatha, U.H.1
-
44
-
-
84921454584
-
Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis
-
44 Sink, R., et al. Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis. J. Med. Chem. 58 (2015), 613–624.
-
(2015)
J. Med. Chem.
, vol.58
, pp. 613-624
-
-
Sink, R.1
-
45
-
-
33846446699
-
Mechanism of thioamide drug action against tuberculosis and leprosy
-
45 Wang, F., et al. Mechanism of thioamide drug action against tuberculosis and leprosy. J. Exp. Med. 204 (2007), 73–78.
-
(2007)
J. Exp. Med.
, vol.204
, pp. 73-78
-
-
Wang, F.1
-
46
-
-
67349287483
-
Synthetic EthR inhibitors boost antituberculous activity of ethionamide
-
46 Willand, N., et al. Synthetic EthR inhibitors boost antituberculous activity of ethionamide. Nat. Med. 15 (2009), 537–544.
-
(2009)
Nat. Med.
, vol.15
, pp. 537-544
-
-
Willand, N.1
-
47
-
-
84959018166
-
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
-
47 Nikiforov, P.O., et al. A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. Org. Biomol. Chem. 14 (2016), 2318–2326.
-
(2016)
Org. Biomol. Chem.
, vol.14
, pp. 2318-2326
-
-
Nikiforov, P.O.1
-
48
-
-
84902438461
-
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches
-
48 Villemagne, B., et al. Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. J. Med. Chem. 57 (2014), 4876–4888.
-
(2014)
J. Med. Chem.
, vol.57
, pp. 4876-4888
-
-
Villemagne, B.1
-
49
-
-
84894266263
-
A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR
-
49 Surade, S., et al. A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR. Biochem. J. 458 (2014), 387–394.
-
(2014)
Biochem. J.
, vol.458
, pp. 387-394
-
-
Surade, S.1
-
50
-
-
6344235517
-
Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis
-
50 Frenois, F., et al. Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis. Mol. Cell 16 (2004), 301–307.
-
(2004)
Mol. Cell
, vol.16
, pp. 301-307
-
-
Frenois, F.1
-
51
-
-
77954600569
-
New molecular scaffolds for the design of Mycobacterium tuberculosis type II dehydroquinase inhibitors identified using ligand and receptor based virtual screening
-
51 Kumar, A., et al. New molecular scaffolds for the design of Mycobacterium tuberculosis type II dehydroquinase inhibitors identified using ligand and receptor based virtual screening. J. Mol. Model. 16 (2010), 693–712.
-
(2010)
J. Mol. Model.
, vol.16
, pp. 693-712
-
-
Kumar, A.1
-
52
-
-
84861563501
-
Elucidation of Mycobacterium tuberculosis type II dehydroquinase inhibitors using a fragment elaboration strategy
-
52 Tran, A.T., et al. Elucidation of Mycobacterium tuberculosis type II dehydroquinase inhibitors using a fragment elaboration strategy. ChemMedChem 7 (2012), 1031–1043.
-
(2012)
ChemMedChem
, vol.7
, pp. 1031-1043
-
-
Tran, A.T.1
-
53
-
-
84860273198
-
Drug design and identification of potent leads against mycobacterium tuberculosis thymidine monophosphate kinase
-
53 Van Calenbergh, S., et al. Drug design and identification of potent leads against mycobacterium tuberculosis thymidine monophosphate kinase. Curr. Top. Med. Chem. 12 (2012), 694–705.
-
(2012)
Curr. Top. Med. Chem.
, vol.12
, pp. 694-705
-
-
Van Calenbergh, S.1
-
54
-
-
84921472546
-
Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors
-
54 Naik, M., et al. Structure guided lead generation for M. tuberculosis thymidylate kinase (Mtb TMK): discovery of 3-cyanopyridone and 1,6-naphthyridin-2-one as potent inhibitors. J. Med. Chem. 58 (2015), 753–766.
-
(2015)
J. Med. Chem.
, vol.58
, pp. 753-766
-
-
Naik, M.1
-
55
-
-
0032508046
-
Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence
-
55 Cole, S.T., et al. Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence. Nature 393 (1998), 537–544.
-
(1998)
Nature
, vol.393
, pp. 537-544
-
-
Cole, S.T.1
-
56
-
-
33646531629
-
The preponderance of P450s in the Mycobacterium tuberculosis genome
-
56 McLean, K.J., et al. The preponderance of P450s in the Mycobacterium tuberculosis genome. Trends Microbiol. 14 (2006), 220–228.
-
(2006)
Trends Microbiol.
, vol.14
, pp. 220-228
-
-
McLean, K.J.1
-
57
-
-
57749112105
-
Characterization of active site structure in CYP121. A cytochrome P450 essential for viability of Mycobacterium tuberculosis H37Rv
-
57 McLean, K.J., et al. Characterization of active site structure in CYP121. A cytochrome P450 essential for viability of Mycobacterium tuberculosis H37Rv. J. Biol. Chem. 283 (2008), 33406–33416.
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 33406-33416
-
-
McLean, K.J.1
-
58
-
-
33846015513
-
Crystal structure of the Mycobacterium tuberculosis P450 CYP121-fluconazole complex reveals new azole drug-P450 binding mode
-
58 Seward, H.E., et al. Crystal structure of the Mycobacterium tuberculosis P450 CYP121-fluconazole complex reveals new azole drug-P450 binding mode. J. Biol. Chem. 281 (2006), 39437–39443.
-
(2006)
J. Biol. Chem.
, vol.281
, pp. 39437-39443
-
-
Seward, H.E.1
-
59
-
-
0036775336
-
Azole antifungals are potent inhibitors of cytochrome P450 mono-oxygenases and bacterial growth in mycobacteria and streptomycetes
-
59 McLean, K.J., et al. Azole antifungals are potent inhibitors of cytochrome P450 mono-oxygenases and bacterial growth in mycobacteria and streptomycetes. Microbiology 148 (2002), 2937–2949.
-
(2002)
Microbiology
, vol.148
, pp. 2937-2949
-
-
McLean, K.J.1
-
60
-
-
84966283595
-
Fragment-based approaches to the development of Mycobacterium tuberculosis CYP121 inhibitors
-
60 Kavanagh, M.E., et al. Fragment-based approaches to the development of Mycobacterium tuberculosis CYP121 inhibitors. J. Med. Chem. 59 (2016), 3272–3302.
-
(2016)
J. Med. Chem.
, vol.59
, pp. 3272-3302
-
-
Kavanagh, M.E.1
-
61
-
-
84883049609
-
Overcoming the limitations of fragment merging: rescuing a strained merged fragment series targeting Mycobacterium tuberculosis CYP121
-
61 Hudson, S.A., et al. Overcoming the limitations of fragment merging: rescuing a strained merged fragment series targeting Mycobacterium tuberculosis CYP121. ChemMedChem 8 (2013), 1451–1456.
-
(2013)
ChemMedChem
, vol.8
, pp. 1451-1456
-
-
Hudson, S.A.1
-
62
-
-
84865835782
-
Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121
-
62 Hudson, S.A., et al. Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121. Angew. Chem. Int. Ed. Engl. 51 (2012), 9311–9316.
-
(2012)
Angew. Chem. Int. Ed. Engl.
, vol.51
, pp. 9311-9316
-
-
Hudson, S.A.1
-
63
-
-
84973573392
-
Spirooxindoles as novel 3D-fragment scaffolds: synthesis and screening against CYP121 from M. tuberculosis
-
63 Davis, H.J., et al. Spirooxindoles as novel 3D-fragment scaffolds: synthesis and screening against CYP121 from M. tuberculosis. Bioorg. Med. Chem. Lett. 26 (2016), 3735–3740.
-
(2016)
Bioorg. Med. Chem. Lett.
, vol.26
, pp. 3735-3740
-
-
Davis, H.J.1
-
64
-
-
50949127310
-
Role of porins for uptake of antibiotics by Mycobacterium smegmatis
-
64 Danilchanka, O., et al. Role of porins for uptake of antibiotics by Mycobacterium smegmatis. Antimicrob. Agents Chemother. 52 (2008), 3127–3134.
-
(2008)
Antimicrob. Agents Chemother.
, vol.52
, pp. 3127-3134
-
-
Danilchanka, O.1
-
65
-
-
84904917797
-
Reactive dirty fragments: implications for tuberculosis drug discovery
-
65 Gopal, P., Dick, T., Reactive dirty fragments: implications for tuberculosis drug discovery. Curr. Opin. Microbiol. 21 (2014), 7–12.
-
(2014)
Curr. Opin. Microbiol.
, vol.21
, pp. 7-12
-
-
Gopal, P.1
Dick, T.2
|