Journal of Heterocyclic Chemistry

Irreversible enzyme inhibitors. CXI. Candidate active??site??directed irreversible inhibitors of dihydrofolic reductase derived from 4, 6??diamino??1, 2??dihydro??l??phenyl??s?? …

BR Baker, MA Johnson

Index: Baker,B.R.; Johnson,M.A. Journal of Heterocyclic Chemistry, 1967 , vol. 4, p. 507 - 510

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Abstract

Abstract Condensation of 5-(p-nitrophenyl)-2-pentanone with phenylbiguanide hydrochloride (V) gave a 2-methyl-2-(p-nitrophenylpropyl)-1, 2-dihydro-s-triazine (IX); hydrogenation of the nitro group to amino followed by bromoacetylation afforded the candidate irreversible inhibitor of dihydrofolic reductase, namely, 2-(p- bromoacetamidophenylpropyl)-4, 6-diamino-1, 2-dihydro-2-methyl-s-triazine ...