Antimycobacterial evaluation of novel [4,5‐dihydro‐1H‐pyrazole‐1‐carbonyl]pyridine derivatives synthesized by microwave‐mediated Michael addition |
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Authors: | Vida Sedighi Parisa Azerang Soroush Sardari |
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Institution: | Drug Design and Bioinformatics Unit, Medical Biotechnology Department, Biotechnology Research Center, Pasteur Institute of Iran, Tehran, Iran |
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Abstract: | The focus of this study is the synthesis and biological activity evaluation of a series of dibenzalaceton derivatives (3a‐3n) and novel 4,5‐dihydro‐1H‐pyrazole‐1‐carbonyl]pyridine derivatives (5a‐5g) against Mycobacterium bovis, Bacillus Calmette–Guerin (BCG). Dibenzalacetone derivatives were synthesized by benzaldehyde derivatives. The 4,5‐dihydro‐1H‐pyrazole‐1‐carbonyl]pyridine derivatives were synthesized by Michael addition reaction and using green chemistry microwave‐mediated method. All compounds were evaluated against BCG and the activity expressed as minimum inhibitory concentration (MIC) in μM. The result showed good activity for all the compounds especially compounds (3a), (3n), and (5a) illustrated high activity (7.03, 8.10 and 5.37 μM, respectively). Copyright © 2014 John Wiley & Sons, Ltd. |
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Keywords: | Mycobacterium BCG synthesis dibenzalaceton derivatives 1H‐pyrazole derivatives |
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