Synthesis of pyrimidine analogs of folic acid
In order to study their antimetabolic activity, we have synthesized the 2-methyl-4-amino-, 2,4-diamino-, 2,6-diamino-4-hydroxy-, and 2,4-dihydroxypyrimidine analogs of folic acid from p-aminobenzoyl-L-glutamic acid and the corresponding substituted 5-bromomethyl-pyrimidines. The high antimetabolic activity of the 2,4-dihydroxypyrimidine analog in the inhibition of the reductases of folic and dihydrofolic acids and of the 2,4-diaminopyrimidine analog in the inhibition of the reductase of dihydrofolic acid has been shown.
KeywordsOrganic Chemistry Folic Acid Pyrimidine Pyrimidine Analog Dihydrofolic Acid
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