Brominated trimetrexate analogues as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase

A Rosowsky, CE Mota…

Index: Rosowsky, Andre; Mota, Clara E.; Queener, Sherry F. Journal of Heterocyclic Chemistry, 1996 , vol. 33, # 6 p. 1959 - 1966

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Citation Number: 24

Abstract

Abstract Five previously undescribed trimetrexate analogues with bulky 2′-bromo substitution on the phenyl ring were synthesized in order to assess the effect of this structure modification on dihydrofolate reductase inhibition. Condensation of 2-[2-(2-bromo-3, 4, 5- trimethoxyphenyl) ethyl]-1, l-dicyanopropene with sulfur in the presence of N, N- diethylamine afforded 2-amino-5-(2′-bromo-3′, 4′, 5′-trimethoxybenzyl)-4-methyl- ...