603955-32-4Relevant academic research and scientific papers
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold
Luo, Qun-Li,Li, Jing-Ya,Liu, Zhi-Ying,Chen, Ling-Ling,Li, Jia,Ye, Qi-Zhuang,Nan, Fa-Jun
, p. 635 - 638 (2005)
Systematic SAR studies on the HTS hit pyridine-2-carboxylic acid thiazol-2-ylamide (PACT) analogues revealed that the scaffold of PCAT is indispensable for the inhibition of type I MetAP. For effective inhibition of the enzyme, the most suitable position to modify is the 3-position of the pyridine ring of PCAT, and the best substituents are those containing O or N atoms connected directly with the pyridine ring. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.
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
Tipparaju, Suresh K.,Joyasawal, Sipak,Pieroni, Marco,Kaiser, Marcel,Brun, Reto,Kozikowski, Alan P.
supporting information; experimental part, p. 7344 - 7347 (2009/12/07)
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
