Salicylanilide carbamates: Antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains

被引：42

作者：

Ferriz, Juana M. ^{[1
]}

Vavrova, Katerina ^{[1
]}

Kunc, Filip ^{[2
,3
]}

Imramovsky, Ales ^{[4
]}

Stolarikova, Jirina ^{[5
]}

Vavrikova, Eva ^{[1
]}

Vinsova, Jarmila ^{[1
]}

机构：

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

[2] Charles Univ Prague, Fac Med, Dept Med Biol, Hradec Kralove 50038, Czech Republic

[3] GENERI BIOTECH, Hradec Kralove 50011, Czech Republic

[4] Univ Pardubice, Fac Chem & Chem Technol, Inst Organ Chem & Technol, Pardubice 53210, Czech Republic

[5] Hlth Inst Ostrava, Lab TBC, Ostrava 70200, Czech Republic

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 03期

关键词：

Salicylanilide carbamates; Multidrug-resistant tuberculosis; In vitro antimycobacterial activity; Cytotoxicity; Chemical hydrolysis; INTERLEUKIN-12P40; PRODUCTION; DRUG DISCOVERY; INHIBITORS; DEGRADATION; DERIVATIVES; PRODRUGS; THERAPY; TARGETS; SYSTEMS; POTENT;

D O I：

10.1016/j.bmc.2009.12.055

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 27 salicylanilide-based carbamates was prepared as a part of our ongoing search for new anti-tuberculosis drugs. These compounds exhibited very good in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium and, in particular, against five multidrug-resistant strains, with MIC values between 0.5-2 mu mol/L. Moreover, they displayed moderate toxicity against intestinal cells with the selectivity index being up to 96. Furthermore, acid stability and a half-life of 43 h at pH 7.4 were shown. Thus, these novel salicylanilide derivatives are drug candidates which should be seriously consider for further screening. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1054 / 1061

页数：8

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