4.4 Article

Synthesis and Evaluation as Antitubercular Agents of 5-Arylethenyl and 5-(Hetero)aryl-3-Isoxazolecarboxylate

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DRUG DEVELOPMENT RESEARCH
卷 74, 期 3, 页码 162-172

出版社

WILEY
DOI: 10.1002/ddr.21057

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Mycobacterium tuberculosis; antituberculosis agents; 3-isoxazolecarboxylic acid alkyl esters

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Preclinical Research 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 (2.311.4M). 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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