Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT)
US5593999A · kind A · utility
Inventors
Key dates
| Filing date | Jun 7, 1995 |
| Grant date | Jan 14, 1997 |
| Priority date | — |
| Expiry date | Jun 7, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D239/95
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Several new 10-formyl and 10-hydroxymethyl derivatives of 5,8,10-trideazapteroic acid are provided, as well as procedures for their preparation. These compounds were shown to be powerful inhibitors of glycinamide ribonucleotide formyltransferase (GARFT), an enzyme that mediates the de novo biosynthesis of purine nucleotides that are required for DNA synthesis and cell division. Due to their ability to interfere with nucleotide biosynthesis and to penetrate microbial cells they are potential anti-microbial agents and are useful for the treatment of opportunistic infections in AIDS and other infections caused by micro-organisms that are resistant to conventional anti-bacterial and anti-fungal agents.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.