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. © 2008 American Chemical Society.
In pursuit of natural product leads: Synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4- carboxylic acid (A-33853) and its analogues: Discovery of N-(2-benzoxazol-2- ylphenyl)benzamides as novel antileishmanial chemotypes / Tipparaju, Suresh K.; Joyasawal, Sipak; Pieroni, Marco; Kaiser, Marcel; Brun, Reto; Kozikowski, Alan P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 51:23(2008), pp. 7344-7347. [10.1021/jm801241n]
In pursuit of natural product leads: Synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4- carboxylic acid (A-33853) and its analogues: Discovery of N-(2-benzoxazol-2- ylphenyl)benzamides as novel antileishmanial chemotypes
PIERONI, Marco;
2008-01-01
Abstract
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. © 2008 American Chemical Society.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
