Acyclic Nucleoside Analogues as Inhibitors of Plasmodium f alciparum dUTPase

…, NG Johansson, D González-Pacanowska…

Index: Nguyen, Corinne; Ruda, Gian Filippo; Schipani, Alessandro; Kasinathan, Ganasan; Leal, Isabel; Musso-Buendia, Alexander; Kaiser, Marcel; Brun, Reto; Ruiz-Perez, Luis M.; Sahlberg, Britt-Louise; Johansson, Nils Gunnar; Gonzalez-Pacanowska, Dolores; Gilbert, Ian H. Journal of Medicinal Chemistry, 2006 , vol. 49, # 14 p. 4183 - 4195

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Citation Number: 54

Abstract

We report the discovery of novel uracil-based acyclic compounds as inhibitors of deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase), an enzyme involved in nucleotide metabolism that has been identified as a promising target for the development of antimalarial drugs. Compounds were assayed against both P. falciparum dUTPase and intact parasites. A good correlation was observed between enzyme inhibition and cellular ...