Thiazolyl-pyrazole derivatives as potential antimycobacterial agents |
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Authors: | Sushma J Takate Abhijit D Shinde Bhausaheb K Karale Hemant Akolkar Laxman Nawale Dhiman Sarkar Pravin C Mhaske |
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Institution: | 1. Department of Chemistry and Research Centre, New Arts, Commerce and Science College, Ahmednagar 414001, India;2. Department of Chemistry, S. P. Mandali’s Sir Parashurambhau College, Tilak Road, Pune 411 030, India;3. Department of Chemistry, Rayat Shikshan Santhsa’s Radhabai Kale Mahila Mahavidyalya, Ahmednagar 414001, India;4. CombiChemBio Resource Centre, National Chemical Laboratory, Pune 411 008, India |
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Abstract: | Mycobacterium tuberculosis (Mtb) is an obligate aerobe that is capable of long-term persistence under conditions of low oxygen tension. A series of thiazolyl-pyrazole derivatives (6a–f, 7a–f, 8c, 8e) were screened for antimycobacterial activity against dormant M. tuberculosis H37Ra (D-MTB) and M. bovis BCG (D-BCG). Nine thiazolyl-pyrazole analogs, 6c, 6e, 7a, 7b, 7c, 7e, 7f, 8c and 8e exhibited promissing minimum inhibitory concentration (MIC) values (0.20–28.25?µg/mL) against D-MTB and D-BCG strains of Mtb. Importantly, six compounds (7a, 7b, 7e, 7f, 8c and 8e) exhibited excellent antimycobacterial activity and low cytotoxicity at the maximum evaluated concentration of >250?µg/mL. Finally, the promising antimycobacterial activity and lower cytotoxicity profile suggested that, these compounds could be further subjected for optimization and development as a lead, which could have the potential to treat tuberculosis. |
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Keywords: | Thiazoles Pyrazole Antimycobacterial activity Cytotoxicity |
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