1. Design and synthesis of novel triazole linked pyrrole derivatives as potent Mycobacterium tuberculosis inhibitors
- Author
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Ravirala Narender, T. Veera Reddy, M. Lakshmi Devi, P. Lakshmi Reddy, Dharmarajan Sriram, Perumal Yogeeswari, and B. V. Subba Reddy
- Subjects
biology ,010405 organic chemistry ,Stereochemistry ,Organic Chemistry ,Isoniazid ,Triazole ,Pyrazinamide ,biology.organism_classification ,01 natural sciences ,Combinatorial chemistry ,0104 chemical sciences ,Mycobacterium tuberculosis ,010404 medicinal & biomolecular chemistry ,Minimum inhibitory concentration ,chemistry.chemical_compound ,chemistry ,medicine ,Click chemistry ,General Pharmacology, Toxicology and Pharmaceutics ,Ethambutol ,Rifampicin ,medicine.drug - Abstract
This research is focused on the rational approach to design and synthesis of a novel series of triazole linked pyrrole derivatives through a sequential Paal–Knorr reaction and Click chemistry. These new molecules were screened against Mycobacterium tuberculosis H37Rv and found to display promising anti-mycobacterial activity. Among various compounds, 7g and 7l were identified as leads with minimum inhibitory concentration value 0.78 (μg/mL), which are more effective than standard drugs such as pyrazinamide, ethambutol, and ciprofloxacin and less active than isoniazid and rifampicin. These molecules (minimum inhibitory concentration values
- Published
- 2017
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