Design and synthesis of novel triazole linked pyrrole derivatives as potent Mycobacterium tuberculosis inhibitors

作者：Devi M Lakshmi; Reddy P Lakshmi; Yogeeswari P; Sriram D; Reddy T Veera^*; Reddy B V Subba^*; Narender R^*

来源：Medicinal Chemistry Research, 2017, 26(11): 2985-2999.

DOI：10.1007/s00044-017-1997-4

• Antitubercular activity
• Stetter reaction
• Paal-Knorr synthesis
• Click chemistry
• Trisubstituted pyrrole derivatives

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 (mu g/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 < 12.5 mu g/mL) were also screened against HEK-293T cancer cell lines. Most of these molecules are less toxic but possess higher selectivity index, which indicates the suitability of these compounds for further evaluation.

• 出版日期2017-11