Irreversible enzyme inhibitors LXXXVII. Hydrophobic bonding to dihydrofolic reductase IX. Mode of binding of m-aryloxyalkyl groups on 4, 6-diamino-1,2-dihydro-2, 2-dimethyl-1-phenyl-s-triazine

Autor: Baker, B.R., Lourens, Gerhardus J.
Zdroj: Journal of Pharmaceutical Sciences; July 1967, Vol. 56 Issue: 7 p871-875, 5p
Abstrakt: The relative binding to dihydrofolic reductase by 16 m-substituted 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-phenyl-s-triazines—nine of which are newly synthesized— has been measured. Strong evidence is presented to indicate that the increased binding by terminal phenyl groups on a m-substituent is due to complexing to a relatively hydrophilic area since terminal benzyl and terminal phenoxy groups give nearly the same increments in binding. The possible conversion of such compounds to candidate active-site-directed irreversible inhibitors of dihydrofolic reductase is discussed.
Databáze: Supplemental Index