The authors declare no conflicts of interest.
Synthesis and Evaluation as Antitubercular Agents of 5-Arylethenyl and 5-(Hetero)aryl-3-Isoxazolecarboxylate
Article first published online: 28 DEC 2012
© 2012 Wiley Periodicals, Inc.
Drug Development Research
Volume 74, Issue 3, pages 162–172, May 2013
How to Cite
Vergelli, C., Cilibrizzi, A., Crocetti, L., Graziano, A., Dal Piaz, V., Wan, B., Wang, Y., Franzblau, S. and Giovannoni, M. P. (2013), Synthesis and Evaluation as Antitubercular Agents of 5-Arylethenyl and 5-(Hetero)aryl-3-Isoxazolecarboxylate. Drug Dev. Res., 74: 162–172. doi: 10.1002/ddr.21057
- Issue published online: 10 APR 2013
- Article first published online: 28 DEC 2012
- Manuscript Accepted: 1 DEC 2012
- Manuscript Received: 24 OCT 2012
- Mycobacterium tuberculosis;
- antituberculosis agents;
- 3-isoxazolecarboxylic acid alkyl esters
A new series of 5-aryl and 5-arylethenylisoxazole carboxylate derivatives was synthesized and evaluated for in vitro activity against Mycobacterium tuberculosis H37Rv. Several compounds exhibited minimum inhibitory concentrations in the low micromolar range (2.3–11.4 μM). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.