Preparation and in-vitro Evaluation of 4-Benzylsulfanylpyridine-2-carbohydrazides as Potential Antituberculosis Agents

被引：6

作者：

Herzigova, Petra ^{[1
]}

Klimesova, Vera ^{[1
]}

Palat, Karel ^{[1
]}

Kaustova, Jarmila ^{[2
]}

Dahse, Hans-Martin ^{[3
]}

Moellmann, Ute ^{[3
]}

机构：

[1] Charles Univ Prague, Fac Pharm, Dept Inorgan & Organ Chem, Hradec Kralove 50005, Czech Republic

[2] Reg Inst Publ Hlth, Lab Mycobacterial Diagnost, Ostrava, Czech Republic

[3] Hans Knoell Inst, Lebniz Inst Nat Stoff Forsch & Infekt Biol eV, Jena, Germany

来源：

ARCHIV DER PHARMAZIE | 2009年 / 342卷 / 07期

关键词：

4-Benzylsulfanyl derivatives; Multidrug-resistant M. tuberculosis; Mycobacterium tuberculosis; Non-tuberculous mycobacteria; Pyridine-2-carbohydrazides; ANTIMYCOBACTERIAL ACTIVITY; BENZIMIDAZOLE DERIVATIVES; DRUGS;

D O I：

10.1002/ardp.200800227

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A set of 4-benzylsulfanylpyridine-2-carbohydrazides was synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, non-tuberculous mycobacteria, and multidrug-resistant M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into a range of 2 to 125 mu mol/L, most often 4 to 32 mu mol/L. The results revealed that the substituents on the benzyl moiety do not influence the antimycobacterial efficacy. The substances exhibited similar activities against sensitive and resistant strains of A tuberculosis. Furthermore, compounds show low antiproliferative effect and cytotoxicity.

引用

页码：394 / 404

页数：11

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