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Titolo:
TETRAZOLE ISOSTERES OF BIOLOGICALLY-ACTIVE ACIDS AND THEIR EFFECTS ONENZYMES
Autore:
KRAUS JL; FAURY P; CHARVET AS; CAMPLO M;
Indirizzi:
FAC SCI LUMINY,CHIM BIOMOLEC LAB,INSERM,U322 F-13288 MARSEILLE 9 FRANCE
Titolo Testata:
Research communications in chemical pathology and pharmacology
fascicolo: 2, volume: 83, anno: 1994,
pagine: 209 - 222
SICI:
0034-5164(1994)83:2<209:TIOBAA>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
MOLECULAR MODIFICATION; DRUG DESIGN; ANALOGS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
26
Recensione:
Indirizzi per estratti:
Citazione:
J.L. Kraus et al., "TETRAZOLE ISOSTERES OF BIOLOGICALLY-ACTIVE ACIDS AND THEIR EFFECTS ONENZYMES", Research communications in chemical pathology and pharmacology, 83(2), 1994, pp. 209-222

Abstract

A number of tetrazole analogs of carboxylic substrates and inhibitorshave been tested. Lactic and pyruvic tetrazoles were found to be competitive inhibitors of rabbit muscle L-lactate dehydrogenase in both the pyruvate reduction and the lactate oxidation reactions (Ki's of 0.04M and 0.08 M D,L-lactic tetrazole and 0.02 M and 0.035 M pyruvic tetrazole, respectively). Lactic tetrazole is a non-competitive inhibitor of yeast L-lactate dehydrogenase (Ki = 0.10 M D,L-lactic tetrazole) while pyruvic tetrazole is predominantly competitive (Ki = 0.15 M). Alanine tetrazole is a poorer substrate than alanine for D-amino acid oxidase. It also acts as weak inhibitor. Benzoic tetrazole is a substrate-competitive inhibitor of D-amino acid oxidase (Ki = 0.7 mM) and is also a stronger ethanol-competitive inhibitor than benzoic acid (Ki = 0.03 M) of liver alcohol dehydrogenase. In all the substrates and inhibitors tested, substitution of a tetrazole ring for a carboxylic group has resulted in decreased binding, presumably due to a dilution of the negative charge density and the larger size of the tetrazoyl anion.

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Documento generato il 31/03/20 alle ore 03:59:16