Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase

…, J Carrero-Lérida, LM Ruiz-Pérez, IH Gilbert…

Index: Cui, Huaqing; Ruda, Gian Filippo; Carrero-Lerida, Juana; Ruiz-Perez, Luis M.; Gilbert, Ian H.; Gonzalez-Pacanowska, Dolores European Journal of Medicinal Chemistry, 2010 , vol. 45, # 11 p. 5140 - 5149

Full Text: HTML

Citation Number: 12

Abstract

Plasmodium falciparum purine nucleoside phosphorylase (PfPNP) has a central role in purine salvage and inhibitors of the enzyme have been shown to have antiplasmodial activity. The enzyme preferentially uses inosine as substrate (Km= 5μM, kcat/Km= 7.4× 104M− 1s− 1), but can also use uridine, albeit less efficiently (Km= 85μM, kcat/Km= 306M− 1s− 1). In an effort to identify new PfPNP inhibitors, two series of compounds were ...