ABSTRACT: 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 microM). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.
Synthesis and evaluation as antitubercular agents of 5-arylethenyl and 5-(hetero)aryl-3-isoxazolecarboxylate / C. Vergelli; A. Cilibrizzi; L. Crocetti; A. Graziano; V. Dal Piaz; B. Wan; Y. Wang; S. Franzblau; MP Giovannoni.. - In: DRUG DEVELOPMENT RESEARCH. - ISSN 0272-4391. - ELETTRONICO. - 74:(2013), pp. 162-172. [10.1002/ddr.21057]
Synthesis and evaluation as antitubercular agents of 5-arylethenyl and 5-(hetero)aryl-3-isoxazolecarboxylate
VERGELLI, CLAUDIA;CROCETTI, LETIZIA;GIOVANNONI, MARIA PAOLA
2013
Abstract
ABSTRACT: 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 microM). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.
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