Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis

Daniele Castagnolo; Marco Radi; Filippo Dessì; Fabrizio Manetti; Manuela Saddi; Rita Meleddu; Alessandro De Logu; Maurizio Botta

doi:10.1016/j.bmcl.2009.02.101

Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2203-5. doi: 10.1016/j.bmcl.2009.02.101. Epub 2009 Feb 28.

Authors

Daniele Castagnolo¹, Marco Radi, Filippo Dessì, Fabrizio Manetti, Manuela Saddi, Rita Meleddu, Alessandro De Logu, Maurizio Botta

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Siena, Italy.

PMID: 19299129
DOI: 10.1016/j.bmcl.2009.02.101

Abstract

A series of novel enantiomerically pure azole derivatives was synthesized. The new compounds, bearing both an imidazole as well as a triazole moiety, were evaluated as antimycobacterial agents. One of them proved to have activity against Mycobaterium tuberculosis comparable to those of the classical antibacterial/antifungal drugs Econazole and Clotrimazole.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Antitubercular Agents / chemical synthesis*
Antitubercular Agents / pharmacology*
Azoles / chemical synthesis*
Azoles / pharmacology*
Drug Evaluation, Preclinical / methods
Microbial Sensitivity Tests / methods
Mycobacterium tuberculosis / drug effects*
Mycobacterium tuberculosis / growth & development*
Stereoisomerism

Substances

Antitubercular Agents
Azoles