TB, caused by Mycobacterium tuberculosis, is one of the deadliest infections worldwide. The co-infection with HIV and the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) strains have further increased the burden for this disease. In the attempt to respond to the constant need of novel therapeutic options, we herein report the discovery of 2,4-diphenyl-1H-imidazoles as effective antitubercular agents, with MIC in the low micromolar range against actively replicating and persistent M. tuberculosis strains. The good activity, along with the lack of toxicity and the feasible synthesis, underscore their value as novel scaffolds for the development of new anti-TB drugs.

Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design / Pieroni, Marco; Wan, Baojie; Zuliani, Valentina; Franzblau, Scott G.; Costantino, Gabriele; Rivara, Mirko. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 100:(2015), pp. 44-49. [10.1016/j.ejmech.2015.05.048]

Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design

PIERONI, Marco;ZULIANI, Valentina;COSTANTINO, Gabriele;RIVARA, Mirko
2015

Abstract

TB, caused by Mycobacterium tuberculosis, is one of the deadliest infections worldwide. The co-infection with HIV and the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) strains have further increased the burden for this disease. In the attempt to respond to the constant need of novel therapeutic options, we herein report the discovery of 2,4-diphenyl-1H-imidazoles as effective antitubercular agents, with MIC in the low micromolar range against actively replicating and persistent M. tuberculosis strains. The good activity, along with the lack of toxicity and the feasible synthesis, underscore their value as novel scaffolds for the development of new anti-TB drugs.
Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design / Pieroni, Marco; Wan, Baojie; Zuliani, Valentina; Franzblau, Scott G.; Costantino, Gabriele; Rivara, Mirko. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 100:(2015), pp. 44-49. [10.1016/j.ejmech.2015.05.048]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2795294
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 19
  • ???jsp.display-item.citation.isi??? 16
social impact