Synthesis and Biological Evaluation of Nonclassical 2, 4-Diamino-5-methylpyrido [2, 3-d] pyrimidines with Novel Side Chain Substituents as Potential Inhibitors of …

A Gangjee, A Vasudevan…

Index: Gangjee, Aleem; Vasudevan, Anil; Queener, Sherry F. Journal of Medicinal Chemistry, 1997 , vol. 40, # 4 p. 479 - 485

Full Text: HTML

Citation Number: 39

Abstract

Nine novel 2, 4-diamino-5-methyl-6-substituted-pyrido [2, 3-d] pyrimidines, 2-10, were synthesized as potential inhibitors of Pneumocystis carinii dihydrofolate reductase (pcDHFR) and Toxoplasma gondii dihydrofolate reductase (tgDHFR). Compounds 2-5 were designed as conformationally restricted analogues of trimetrexate (TMQ), in which rotation around τ3 was constrained by incorporation of the side chain nitrogen as part of an ...