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Titolo:
EPOXYETHANE- ETHYNESULFONAMIDES WITH ANTIFILARIAL ACTIVITIES - DEGRADATION KINETICS AND INHIBITORY EFFECT ON FILARIAL MALATE-DEHYDROGENASE AND LACTATE-DEHYDROGENASE/
Autore:
RADEMBINO N; LOISEAU PM; DESSALLES MC; MARCHAT L; BORIES C; GAYRAL P; MAHUZIER G;
Indirizzi:
FAC PHARM,PARASITOL LAB,5 RUE JEAN BAPTISTE CLEMENT F-92296 CHATENAY MALABR FRANCE FAC PHARM,PARASITOL LAB F-92296 CHATENAY MALABR FRANCE FAC PHARM,LAB METHODOL BIOANALYT F-92296 CHATENAY MALABR FRANCE
Titolo Testata:
Arzneimittel-Forschung
fascicolo: 3, volume: 48, anno: 1998,
pagine: 294 - 299
SICI:
0004-4172(1998)48:3<294:EEWAA->2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
MOLINEMA-DESSETAE NEMATODA; FILARIOIDEA;
Keywords:
EPOXYETHANESULFONAMIDES, DEGRADATION KINETICS, STABILITY; ETHYNESULFONAMIDES, DEGRADATION KINETICS, STABILITY; FILARIAL ENZYMES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
10
Recensione:
Indirizzi per estratti:
Citazione:
N. Radembino et al., "EPOXYETHANE- ETHYNESULFONAMIDES WITH ANTIFILARIAL ACTIVITIES - DEGRADATION KINETICS AND INHIBITORY EFFECT ON FILARIAL MALATE-DEHYDROGENASE AND LACTATE-DEHYDROGENASE/", Arzneimittel-Forschung, 48(3), 1998, pp. 294-299

Abstract

Some epoxyethane-/ethynesulfonamides had shown strong filaricidal activity with inconstant reproducibility as a result of a lack of stability in aqueous solution. The degradation in hydroxylic and aprotic solutions of two epoxyethanesulfonamides and one ethynesulfonamide was investigated using TLC, HPLC, GC and mass spectrometry. For both epoxydes, the degradation rate followed first-order kinetics and was more rapid in hydroxylic than in aprotic solutions. The degradation increased with the temperature whereas it was not modified with and without lightexposure. Four kinds of degradation products were found: the first one involved the oxidation of the epoxyde bond, the second the breaking of the N-S bond, the third a desulfonation product and the fourth was not identified. In contrast, the stability of ethynesulfonamide was better than those of epoxyethanesulfonamide. These results suggest that epoxyethanesulfonamides should be kept at + 4 degrees C before being injected to animals during the study of biological activity. Since epoxyde compounds are known to have inhibitory effects on parasite energy metabolism enzymes, the compounds were evaluated on two major filarialenzymes: lactate dehydrogenase (LDH) and cytoplasmic malate dehydrogenase (MDH). Both epoxyethanesulfonamides showed only a slight inhibitory effect on filarial LDH and MDH confirming the evidence that the main mode of action of these compounds remains to discover. Moreover, ethynesulfonamide and the degradation products of both epoxyethanesulfonamides had no effect on LDH and MDH.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/07/20 alle ore 15:34:29