The synthesis and antimycobacterial properties of 4-(substituted benzylsulfanyl)pyridine-2-carboxamides

被引:1
作者
Klimesova, Vera [1 ]
Herzigova, Petra [1 ]
Palat, Karel [1 ]
Machacek, Milos [1 ]
Stolarikova, Jirina [2 ]
Dahse, Hans-Martin [3 ]
Moellmann, Ute [3 ]
机构
[1] Charles Univ Prague, Fac Pharm, Dept Inorgan & Organ Chem, Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic
[2] Reg Inst Publ Hlth, Ostrava 70200, Czech Republic
[3] Hans Knoell Inst, Leibniz Inst Nat Prod Res & Infect Biol, D-07745 Jena, Germany
关键词
4-Benzylsulfanyl derivatives; pyridine-2-carboxamides; antimycobacterial activity; cytotoxicity;
D O I
10.3998/ark.5550190.0013.308
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
4-(Substituted benzylsulfanyl)pyridine-2-carboxamides 6 were synthesized by a three-step synthesis starting from 4-chloropyridine-2-carboxylic acid and substituted benzyl thiols, with the exception of nitroderivatives. The compounds were evaluated for their anti-TB activity against M. tuberculosis, non-tuberculous mycobacteria (M. kansasii and M. avium), and MDR strains of M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into the range of 8-250 mu mol/L. The substances exhibited similar activities against both sensitive and resistant strains.
引用
收藏
页码:90 / 103
页数:14
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