Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents
| Autor: | Amol S. Shah, Shankar G. Alegaon, Pranali V. Sonkusare, Sagar M. Chaudhary, Kallanagouda R. Alagawadi, Dilip H. Dadwe |
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| Rok vydání: | 2011 |
| Předmět: |
Rhodanine
Stereochemistry medicine.drug_class Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Acetates Antimycobacterial Biochemistry Microwave assisted Mycobacterium tuberculosis Acetic acid chemistry.chemical_compound Drug likeness Drug Discovery Thiadiazoles medicine Humans Tuberculosis Molecular Biology Trifluoromethyl biology Chemistry Organic Chemistry Imidazoles biology.organism_classification Combinatorial chemistry Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 22(5) |
| ISSN: | 1464-3405 |
| Popis: | The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacterium tuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6-arylimidazo[2,1- b ][1,3,4]thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M . tuberculosis H 37 Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12–1.56 μg/ml. The present study suggests that compounds 6b , 6c , 6d , 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents. |
| Databáze: | OpenAIRE |
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