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Titolo:
SELECTIVE AND POTENT MONOAMINE-OXIDASE TYPE-B INHIBITORS - SUBSTITUTED SEMICARBAZONES AND ACYLHYDRAZONES OF AROMATIC-ALDEHYDES AND KETONES
Autore:
BERNARD S; PAILLAT C; ODDOS T; SEMAN M; MILCENT R;
Indirizzi:
UNIV PARIS 07,FAC MED XAVIER BICHAT,UNITE RECH CHIM & PHARMACOL,CHIM ORGAN MED LAB F-75870 PARIS 18 FRANCE UNIV PARIS 07,FAC MED XAVIER BICHAT,UNITE RECH CHIM & PHARMACOL,CHIM ORGAN MED LAB F-75870 PARIS 18 FRANCE LAB MAYOLY SPINDLER F-78401 CHATOU FRANCE UNIV PARIS 07,IMMUNODIFFERENCIAT CELLULAIRE LAB F-75251 PARIS 05 FRANCE
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 6, volume: 30, anno: 1995,
pagine: 471 - 482
SICI:
0223-5234(1995)30:6<471:SAPMTI>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
PARKINSONS-DISEASE; BINDING; DERIVATIVES; ANALOGS; BEHAVIOR;
Keywords:
MAO B INHIBITOR; HYDRAZONE (AROMATIC ACYL-); SEMICARBAZONE (AROMATIC);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
S. Bernard et al., "SELECTIVE AND POTENT MONOAMINE-OXIDASE TYPE-B INHIBITORS - SUBSTITUTED SEMICARBAZONES AND ACYLHYDRAZONES OF AROMATIC-ALDEHYDES AND KETONES", European journal of medicinal chemistry, 30(6), 1995, pp. 471-482

Abstract

The synthesis and the evaluation of the monoamine oxidase A and B inhibitory activities of 21 new substituted acylhydrazones of various aromatic aldehydes and 4-(benzyloxy)acetophenone, and four substituted semicarbazones of benzaldehyde and 4-(benzyloxy)benzaldehyde, are described. The 4-(benzyloxy)phenyl group contributing to a high lipophilicity led to the most active compounds. One of these, compound 3g (IC50 = 3 nM, MAO A/MAO B selectivity > 33 000), was found to act as a reversible and probably tight-binding inhibitor. The studied acyclic hydrazones and semicarbazones are structurally related to other reversible andpotent inhibitors, eg, heterocyclic compounds such as 1,3,4-oxadiazol-2(3H)-one derivatives in which the hydrazono group is intracyclic. Some of these new inhibitors might find use in the symptomatic treatmentof neurodegenerative processes.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 19:26:50