Journal of Heterocyclic Chemistry

Analogs of tetrahydrofolic acid. XII. On the relative contribution by the 2??amino and 4??hydroxy groups of 2??amino??5??(3??anilinopropyl)??6??methyl??4??pyrimidinol to …

BR Baker, BT Ho, T Neilson

Index: Baker,B.R. et al. Journal of Heterocyclic Chemistry, 1964 , vol. 1, p. 79 - 87

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Citation Number: 36

Abstract

Abstract The structure of 2-amino-5-(3-anilinopropyl)-6-methyl-4-pyrimidinol (II), an inhibitor of both dihydrofolic reductase and thymidylate synthetase, has been modified by replacement of the 2-amino group by hydrogen or the 4-hydroxyl group by hydrogen, mercapto or amino. Enzymic evaluation showed that 5-(3-anilinopropyl)-2, 4-diamino-6- methyl-pyrimidine was a 170-fold more effective inhibitor of dihydrofolic reductase than ...