Non-classical folate analogue inhibitors of glycinamide ribonucl

Details Non-classical folate analogue inhibitors of glycinamide ribonucl Non-classical folate analogue inhibitors of glycinamide ribonucl

1995-06-07

1997-01-14

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544284, 544287, C07D40106, C07D40906, C07D40506, C07D23990

Patent

active

055939996

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.

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Nair et al. "Synthesis of the reduced derivatives of 11-deazahomofolic acid . . . inhibitors of GARFT" J. Med. Chem. 32, 1277 (1989) month of publication not provided.
Nair et al. Inhibitors of glycinamide ribonucleotide formyltransferase GARFT. Drugs of the Future. 18(4):335-342 (1993) month of publication not provided.

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