期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 100, 期 -, 页码 223-234出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.06.007
关键词
Tuberculosis; FabG4; HtdX; MIC; Biofilm; Polypharmacology
资金
- Council of Scientific and Industrial Research (CSIR) [02(0014)/11/EMR-II]
- DBT [BT/PR14496/MED/30/550/2010]
- IIT Kharagpur [IIT/SRIC/BIO/LDO/2014-15/33]
- DST
Herein, we present dual inhibitors of new targets FabG4 and HtdX for the first time. In this work, eight compounds have been designed, synthesized, characterized and evaluated for bio-activities. Amongst them, six compounds have shown inhibitory activities. Three of them (12-14) demonstrate dual inhibition of both FabG4 and HtdX at low micromolar concentration. In addition, the dual inhibitors show good anti-mycobacterial properties against both planktonic growth and biofilm culture of Mycobacterium species. This study is an important addition to tuberculosis drug discovery because it explores two new enzymes as drug targets and presents their dual inhibitors as good candidates for pre-clinical trials. (C) 2015 Elsevier Masson SAS. All rights reserved.
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