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Synthesis and Evaluation as Antitubercular Agents of 5‐Arylethenyl and 5‐(Hetero)aryl‐3‐Isoxazolecarboxylate
Author(s) -
Vergelli Claudia,
Cilibrizzi Agostino,
Crocetti Letizia,
Graziano Alessia,
Dal Piaz Vittorio,
Wan Baojie,
Wang Yuehong,
Franzblau Scott,
Giovani Maria Paola
Publication year - 2013
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21057
Subject(s) - isoxazole , aryl , chemistry , in vitro , stereochemistry , ring (chemistry) , combinatorial chemistry , pharmacology , organic chemistry , biochemistry , biology , alkyl
Preclinical ResearchA new series of 5‐aryl and 5‐arylethenylisoxazole carboxylate derivatives was synthesized and evaluated for in vitro activity against M ycobacterium tuberculosis H 37 R v . Several compounds exhibited minimum inhibitory concentrations in the low micromolar range (2.3–11.4 μ M ). A variety of substituents introduced around the isoxazole ring allowed the delineation of preliminary SARs for this new series of compounds.