期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 3, 页码 1054-1061出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.055
关键词
Salicylanilide carbamates; Multidrug-resistant tuberculosis; In vitro antimycobacterial activity; Cytotoxicity; Chemical hydrolysis
资金
- MSM [0021620822]
- GAUK [76807/2007]
- IGA NS [10367-3]
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.
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