In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazol e-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as Novel

[摘要]：The antibiotic A 33853 I (R = 3-hydroxy-2-pyridinyl; R1 = HO), an acylaminophenylbenzooxazolecarboxylic acid, a potential antileishmanial agent, is prepd. for the first time; analogous acylaminophenylbenzooxazolecarboxylic acids I [R = 2-pyridinyl, 3=fluoro-2-pyridinyl, 2-HOC6H4, 3-ClC6H4, 3-pyridinyl, 2-chloro-3-pyridinyl, 2,3,4-F3C6H2, 3,4,5-(HO)3C6H2, Ph, pyrazinyl, 1H-indol-2-yl, 2-phenyl-4-quinolinyl, 5-phenyl-3-isoxazolyl, 5-methyl-3-isoxazolyl; R1 = H, MeO, HO] are prepd. and tested as antileishmanial agents. I (R = 3-hydroxy-2-pyridinyl; R1 = HO) inhibits the growth of L. donovani roughly three times more effectively than the known antileishmanial agent miltefosine; I (R = 2-pyridinyl, 3-fluoro-2-pyridinyl, pyrazinyl; R1 = HO) inhibit the growth of L. donovani with IC50 values of 0.31-0.52 mM while being cytotoxic to L6 rat skeletal cells at IC50 values of 31-204 mM (selectivity indexes of 99-392).

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