Banerjee, Deb Ranjan ; Biswas, Rupam ; Das, Amit K. ; Basak, Amit (2015) Design, synthesis and characterization of dual inhibitors against new targets FabG4 and HtdX of Mycobacterium tuberculosis European Journal of Medicinal Chemistry, 100 . pp. 223-234. ISSN 0223-5234
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Official URL: http://doi.org/10.1016/J.Ejmech.2015.06.007
Related URL: http://dx.doi.org/10.1016/J.Ejmech.2015.06.007
Abstract
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.
Item Type: | Article |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | Tuberculosis; FabG4; HtdX; MIC; Biofilm; Polypharmacology |
ID Code: | 130024 |
Deposited On: | 02 Dec 2022 06:01 |
Last Modified: | 05 Dec 2022 05:44 |
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