Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase

…, L Maes, LM Ruiz-Perez, DG Pacanowska…

Index: Chowdhury, Shafinaz F.; Villamor, Victor Bernier; Guerrero, Ramon Hurtado; Leal, Isabel; Brun, Reto; Croft, Simon L.; Goodman, Jonathan M.; Maes, Louis; Ruiz-Perez, Luis M.; Pacanowska, Dolores Gonzalez; Gilbert, Ian H. Journal of Medicinal Chemistry, 1999 , vol. 42, # 21 p. 4300 - 4312

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Citation Number: 79

Abstract

This paper concerns the design, synthesis, and evaluation of inhibitors of leishmanial and trypanosomal dihydrofolate reductase. Initially study was made of the structures of the leishmanial and human enzyme active sites to see if there were significant differences which could be exploited for selective drug design. Then a series of compounds were synthesized based on 5-benzyl-2, 4-diaminopyrimidines. These compounds were assayed against the ...