Structural studies on bioactive compounds. 8. Synthesis, crystal structure and biological properties of a new series of 2, 4-diamino-5-aryl-6-ethylpyrimidine …

…, MA Meek, CH Schwalbe, MFG Stevens

Index: Griffin, Roger J.; Meek, Michelle A.; Schwalbe, Carl H.; Stevens, Malcolm F. G. Journal of Medicinal Chemistry, 1989 , vol. 32, # 11 p. 2468 - 2474

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Citation Number: 19

Abstract

A series of 2, 4-diamino-5-aryl-6-ethylpyrimidines embracing basic substituents in the 5-aryl ring was synthesized and evaluated for inhibitory activity against rat liver dihydrofolate reductase (DHFR). Maximal enzyme inhibition was observed for compounds bearing a benzylamino (19) or N-alkylbenzylamino substituent (29 and 30) in the 4-position of the phenyl ring and a nitro group in the 3-position, the corresponding 3-amino, 3-azido, or ...