Inventors:
Stephen J. Benkovic - State College PA
Richard A. Blatchly - Shelburne Falls MA
James Inglese - E. Hanover NJ
Assignee:
The Pennsylvania State University - State College PA
International Classification:
C07H 906
A61K 3170
A61K 31395
Abstract:
The present invention is directed to several multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase (GAR TFase; E. C. 2. 1. 2. 2), a folate-requiring enzyme of de novo purine biosynthesis. The compounds of the present invention will be useful to provide anti-gout and/or anti-neoplastic therapeutic agents or will serve as potentiators for other such agents. The most prefeffed, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N. sup. 10 -[5'-phosphoribosyl-1'-. beta. -aminocarbonylmethyl-1-thioacetyl]-5,8-dideaz afolate, which has the chemical formula: ##STR1##.