Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 9, Pages 2245-2250Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.03.059
Keywords
Benzo[d]isoxazole; Piperazine; Homopiperazine; Indole; Triazole; Mycobacterium tuberculosis; Anti-tubercular agents
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Funding
- DST, New Delhi, India [SB/S1/OC-60/2013]
- BITS-Pilani, Hyderabad Campus
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A series of thirty eight novel 3-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl/1,4-diazepan-1-yl)benzo[d]isoxazole and 1-(4-(benzo[d]isoxazol-3-yl)piperazin-1-yl/1,4-diazepan-1-yl)-2-(1H-indol-3-yl) substituted-1-one analogues were synthesised, characterised using various analytical techniques and evaluated for in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain and two 'wild' strains Spec. 210 and Spec. 192. The titled compounds exhibited minimum inhibitory concentration (MIC) ranging from 6.16 to > 200 mu M. Among the tested compounds, 7i, 7y and 7z exhibited moderate activity (MIC = 24.03 -29.19 mu M) and 7j exhibited very good anti-tubercular activity (MIC = 6.16 mu M). Furthermore, 7i, 7j, 7y and 7z were found to be non-toxic against mouse macrophage cell lines when screened for toxicity. All the synthesised compounds were docked to pantothenate synthetase enzyme site to know deferent binding interactions with the receptor. (C) 2016 Elsevier Ltd. All rights reserved.
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