Optimization of potent inhibitors of P. falciparum dihydroorotate dehydrogenase for the treatment of malaria

…, RH Barker Jr, CA Celatka, TJ O'Shea…

文献索引：Skerlj, Renato T.; Bastos, Cecilia M.; Booker, Michael L.; Kramer, Martin L.; Barker, Robert H.; Celatka, Cassandra A.; O'Shea, Thomas J.; Munoz, Benito; Sidhu, Amar Bir; Cortese, Joseph F.; Wittlin, Sergio; Papastogiannidis, Petros; Angulo-Barturen, Inigo; Jimenez-Diaz, Maria Belen; Sybertz, Edmund ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 9 p. 708 - 713

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被引用次数: 24

摘要

Inhibition of dihydroorotate dehydrogenase (DHODH) for P. falciparum potentially represents a new treatment option for malaria, since DHODH catalyzes the rate-limiting step in the pyrimidine biosynthetic pathway and P. falciparum is unable to salvage pyrimidines and must rely on de novo biosynthesis for survival. We report herein the synthesis and structure–activity relationship of a series of 5-(2-methylbenzimidazol-1-yl)-N- ...