Design, synthesis and evaluation of 2, 4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase

…, R Brun, LMR Pérez, D González-Pacanowska…

文献索引：Khabnadideh, Soghra; Pez, Didier; Musso, Alexander; Brun, Reto; Ruiz Perez, Luis M.; Gonzalez-Pacanowska, Dolores; Gilbert, Ian H. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 7 p. 2637 - 2649

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被引用次数: 55

摘要

This paper describes the design, synthesis and evaluation of a series of 2, 4- diaminoquinazolines as inhibitors of leishmanial and trypanosomal dihydrofolate reductase. Compounds were designed by a generating virtual library of compounds and docking them into the enzyme active site. Following their synthesis, they were found to be potent and selective inhibitors of leishmanial dihydrofolate reductase. The compounds were also ...