Inhibition of chicken liver 5-aminoimidazole-4-carboxamide ribonucleotide transformylase by 5,8-dideaza analogues of folic acid

W. Thomas Mueller, Gary K. Smith, Stephen J. Benkovic, John B. Hynes

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5 Scopus citations

Abstract

A series of fourteen 5,8-dideaza analogues of folic and pteroic acids was evaluated for inhibition of 5-aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR TFase) from chicken liver. Of the 5,8-dideaza folate derivatives studied, 10-oxa-5,8-dideazafolic acid was the most potent inhibitor. The addition of one l-glutamate moiety to the γ-carboxyl group caused a 6- to 7-fold reduction in Ki in three instances. Two compounds devoid of an l-glutamate were 4- to 6-fold less inhibitory than their parent counterparts possessing one l-glutamate residue.

Original languageEnglish (US)
Pages (from-to)449-451
Number of pages3
JournalBiochemical Pharmacology
Volume37
Issue number3
DOIs
StatePublished - Feb 1 1988

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Pharmacology

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