Chemical and Biological Studies on 1,2-Dihydro-s-triazines. V. Inhibition of Derivatives of Pteroylglutamic Acid

TLDR: The phenyl- and 3′- and 4′- halophenyl-2,2-dimethyl derivatives were the most active compounds of the series and certain correlations can be made between structure and microbiological activity vs these metabolites.

Abstract: SummaryDihydropteroylglutamic acid, N10-formylpteroylglutamic acid and citro vorum factor are inhibited non-competitively by a number of 1,2-dihydro-s-triazines when substituted for pteroylglutamic acid in 5. faecalis No. 8043 assay systems, but only by inhibitor:metabolite ratios considerably higher than those required for the inhibition of pteroylglutamic acid in the same microbiological system. Citrovorum factor also is similarly inhibited in L. citrovorum No. 8081 assay systems. The phenyl- and 3′- and 4′- halophenyl-2,2-dimethyl derivatives were the most active compounds of the series and certain correlations can be made between structure and microbiological activity vs these metabolites.