2, 4-Diaminopyrimidines as inhibitors of leishmanial and trypanosomal dihydrofolate reductase

…, I Leal, F Zuccotto, C Boussard, R Brun, SL Croft…

Index: Pez, Didier; Leal, Isabel; Zuccotto, Fabio; Boussard, Cyrille; Brun, Reto; Croft, Simon L.; Yardley, Vanessa; Ruiz Perez, Luis M.; Gonzalez Pacanowska, Dolores; Gilbert, Ian H. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4693 - 4711

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Citation Number: 52

Abstract

This paper describes the synthesis of 4′-substituted and 3′, 4′-disubstituted 5-benzyl-2, 4-diaminopyrimidines as selective inhibitors of leishmanial and trypanosomal dihydrofolate reductase. Compounds were then assayed against the recombinant parasite and human enzymes. Some of the compounds showed good activity. They were also tested against the intact parasites using in vitro assays. Good activity was found against Trypanosoma cruzi, ...