Journal of pharmaceutical sciences

Irreversible enzyme inhibitors LXXI. Candidate active??site??directed irreversible inhibitors of dihydrofolic reductase V. Derivatives of 6??phenylpyrimidine

BR Baker, HS Shapiro

Index: Baker,B.R.; Santi,D.V. Journal of Pharmaceutical Sciences, 1967 , vol. 56, p. 380 - 384

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Citation Number: 6

Abstract

Abstract A series of 2-amino-5-anilinopropyl-6-phenyl-4-pyrimidinols bearing p-chloroacetyl (Va), p-(4-chloro-3-butanon-1-yl)(Vb),-(4-chloro-1-buten-3-one-1-yl)(Vc), and p- bromoacetamidoethyl (IVd) groups on the anilino moiety were synthesized as candidate active-site-directed irreversible inhibitors of dihydrofolic reductase. Only Vb inactivated dihydrofolic reductase when they were incubated together at 37; the half-life was about 60 ...