New 2, 4-diamino-5-(2', 5'-substituted benzyl) pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and …

A Rosowsky, RA Forsch, CH Sibley…

Index: Rosowsky, Andre; Forsch, Ronald A.; Sibley, Carol Hopkins; Inderlied, Clark B.; Queener, Sherry F. Journal of Medicinal Chemistry, 2004 , vol. 47, # 6 p. 1475 - 1486

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Citation Number: 44

Abstract

In a continuing effort to design small-molecule inhibitors of dihydrofolate reductase (DHFR) that combine the enzyme-binding selectivity of 2, 4-diamino-5-(3', 4', 5'-trimethoxybenzyl) pyrimidine (trimethoprim, TMP) with the potency of 2, 4-diamino-5-methyl-6-(2', 5'- dimethoxybenzyl) pyrido [2, 3-d] pyrimidine (piritrexim, PTX), seven previously undescribed 2, 4-diamino-5-[2'-methoxy-5'-(substituted benzyl)] pyrimidines were synthesized in which ...