In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-3-hydroxy-2-(3-hydroxypyridine-2-carbonyl)aminophenylbenzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as No

Tipparaju  SK; Joyasawal  S; Pieroni  MKaiser  MBrun  RKozikowski  AP

首页> 外文期刊>Journal of Medicinal Chemistry >In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-3-hydroxy-2-(3-hydroxypyridine-2-carbonyl)aminophenylbenzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as No

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In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-3-hydroxy-2-(3-hydroxypyridine-2-carbonyl)aminophenylbenzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as No

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The first synthesis and biological evaluation of antibiotic 31 (A-33853) and its analogues are reported. Initial screening for inhibition of L. donovani, T. b. rhodesiense, T cruzi, and P. falciparum cultures followed by determination of IC50 in L. donovani and cytotoxicity on L6 cells revealed 31 to be 3-fold more active than miltefosine, a known antileishmanial drug, Compounds 14, 15, and 25 selectively inhibited L. donovani at nanomolar concentrations and showed much lower cytotoxicity.

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《Journal of Medicinal Chemistry》 |2008年第23期|7344-7347|共4页
作者
Tipparaju SK; Joyasawal S; Pieroni MKaiser MBrun RKozikowski AP;
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[Tipparaju, SK;

Joyasawal, S;

Pieroni, MKozikowski, AP] Univ Illinois, Dept Med Chem & Pharmacognosy, Drug Discovery Program, Chicago, IL 60612 USA[Kaiser, MBrun, R] Swiss Trop Inst, CH-4002 Basel, Switzerland;

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正文语种英语
中图分类药学;
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ANTHRACIS ENOYL-ACP; VISCERAL LEISHMANIASIS; MILTEFOSINE; INHIBITORS; REDUCTASE; DESIGN;

In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-3-hydroxy-2-(3-hydroxypyridine-2-carbonyl)aminophenylbenzoxazole-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as No

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