GAR transformylase inhibitor
US4999424A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 10, 1988 |
| Grant date | Mar 12, 1991 |
| Priority date | — |
| Expiry date | Nov 10, 2008 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H13/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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##
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.