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

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

文献索引：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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被引用次数: 79

摘要

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 ...