Remember Me
Or use your Academic/Social account:


Or use your Academic/Social account:


You have just completed your registration at OpenAire.

Before you can login to the site, you will need to activate your account. An e-mail will be sent to you with the proper instructions.


Please note that this site is currently undergoing Beta testing.
Any new content you create is not guaranteed to be present to the final version of the site upon release.

Thank you for your patience,
OpenAire Dev Team.

Close This Message


Verify Password:
Verify E-mail:
*All Fields Are Required.
Please Verify You Are Human:
fbtwitterlinkedinvimeoflicker grey 14rssslideshare1
Bhakta, Sanjib (2016)
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.
  • The results below are discovered through our pilot algorithms. Let us know how we are doing!

    • 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.
  • Inferred research data

    The results below are discovered through our pilot algorithms. Let us know how we are doing!

    Title Trust
  • Discovered through pilot similarity algorithms. Send us your feedback.

Share - Bookmark

Funded by projects

  • RCUK | ATP-dependent Mur ligases ...
  • WT

Cite this article