Summary A series of 1,2-dihydro-
s-triazines has been studied in
Lactobacillus casei # 7469-pteroylglutamic acid systems. The active derivatives exhibit a competitive inhibition similar to that of 4-aminopteroylglutamic
acid, but differ from the latter in that inhibition is not relieved by adenine or guanine, and at appropriate concentrations
of inhibitor, is not reversed by excess pteroylglutamic acid. Differences in microbiological activity can be correlated with
certain alterations in the structure of the molecule, maximum activity being exhibited by the 2,2-dimethyl-phenyl- and 2,2-dimethyl-
m-chlorophenyl derivatives.
The inhibitory effect of these compounds is reversed·by appropriate concentrations of dihydropteroylglutamic acid, N
10-formylpteroylglutamic acid, synthetic and natural citrovorum factor, thymine and thymidine. The similarity in inhibition
indices obtained vs the various forms of pteroylglutamic acid in
Lactobacillus casei bioassay systems and the correlation with those vs citrovorum factor in
Streptococcus faecalis # 8043 and
Leuconostoc citrovorum # 8081 bioassay systems suggests that inhibition of
Lactobacillus casei is the result of interference with the utilization of citrovorum factor.
Part I: J. Amer. Chem. Soc.
74, 855, 1952; Amer. J. Path.
28, 599, 1952; II: J. Amer. Chem. Soc. 1955, in press; III: J. Amer. Chem. Soc. 1955, in press; IV: Proc. Soc. Exp. Biol. Med.
83, 733, 1953; V: Proc. Soc. Exp. Biol. Med.
83, 740, 1953; VI: Proc. Soc. Exp. Biol. Med.
83, 742, 1953.
The experimental work for this and studies VIII, IX, and X in this series was done in part at the Laboratorium voor de Gezondheidscleer,
Universiteit van Amsterdam, Nederland, which is directed by Professor Dr
A. Charlotte Ruys, and these four reports are based upon a thesis submitted by G.E.F. to the Faculteit der Wis-en Natuurkunde, in partial fulfiment
of the requirements for the degree of Doctor of Science.
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