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fbtwitterlinkedinvimeoflicker grey 14rssslideshare1
Publisher: American Chemical Society
Languages: English
Types: Article
Subjects: bcs
Novel pyrroles have been designed, synthesized and evaluated against mycobacterial strains. The pyrroles have originally been designed as hybrids of the anti-tubercular drugs BM212 1 and SQ109 2 that showed common chemical features with very similar topological distribution. A perfect superposition of the structures of 1 and 2 revealed by computational studies suggested the introduction of bulky substituents at the terminal portion of the pyrrole C3 side chain and the removal of the C5 aryl moiety. Five compounds showed high activity toward Mycobacterium tuberculosis, while 9b and 9c were highly active also against multi-drug resistant clinical isolates. Compound 9c showed low eukaryotic cell toxicity, turning out to be an excellent lead candidate for preclinical trials. In addition, four compounds showed potent inhibition (comparable to that of verapamil) towards the whole-cell drug efflux pump activity of mycobacteria, and thus turning to be promising multi-drug resistance reversal agents.
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    • 1. WHO. Global tuberculosis report http://www.who.int/tb/publications/global_report/en/ (accessed February 08th, 2016). 4. Eker, B.; Ortmann, J.; Migliori, G. B.; Sotgiu, G.; Muetterlein, R.; Centis, R.; Hoffmann, H.; Kirsten, D.; Schaberg, T.; Ruesch-Gerdes, S.; Lange, C. Multidrug- and extensively drugresistant tuberculosis, Germany. Emerging Infect. Dis. 2008, 14, 1700-1706. 5. Mitnick, C.D.; Shin, S. S.; Seung, K. J.; Rich, M. L.; Atwood, S.S.; Furin, J. J.; Fitzmaurice, G. M.; Alcantara Viru, F. A.; Appleton, S. C.; Bayona, J. N.; Bonilla, C. A.; Chalco, K.; Choi, S.; Franke, M. F.; Fraser, H. S.; Guerra, D.; Hurtado, R. M.; Jazayeri, D.; 21. Wermuth, C. G., Aldous, D., Raboisson, P., Rognan, D., Eds.; The Practice of Medicinal Chemistry, 4th ed.; Academic Press: London, 2015; p 385.
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