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Titolo:
NOVEL [2-(4-PIPERIDINYL)ETHYL](THIO)UREAS - SYNTHESIS AND ANTIACETYLCHOLINESTERASE ACTIVITY
Autore:
VIDALUC JL; CALMEL F; BIGG D; CARILLA E; STENGER A; CHOPIN P; BRILEY M;
Indirizzi:
CTR RECH PIERRE FABRE MEDICAMENT,DIV MED CHEM,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE CTR RECH PIERRE FABRE MEDICAMENT,DIV NEUROBIOL F-81106 CASTRES FRANCE
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 5, volume: 37, anno: 1994,
pagine: 689 - 695
SICI:
0022-2623(1994)37:5<689:N[-SAA>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
SCOPOLAMINE-INDUCED AMNESIA; BETA-AMYLOID PRECURSOR; ALZHEIMERS-DISEASE; SENILE DEMENTIA; PIPERIDINE-DERIVATIVES; CHOLINERGIC NEURONS; ACETYLCHOLINESTERASE; INHIBITORS; BRAIN; ISOTHIOCYANATES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
60
Recensione:
Indirizzi per estratti:
Citazione:
J.L. Vidaluc et al., "NOVEL [2-(4-PIPERIDINYL)ETHYL](THIO)UREAS - SYNTHESIS AND ANTIACETYLCHOLINESTERASE ACTIVITY", Journal of medicinal chemistry, 37(5), 1994, pp. 689-695

Abstract

A series of 1-ar(o)yl-3- [2-(1-benzyl-4-piperidinyl)ethyl] (thio)ureaderivatives was synthesized and evaluated for antiacetylcholinesterase activity. Most aroyl(thio)urea derivatives showed potent inhibitory activity in the sub-micromolar range. A comparable potency was obtained with the aryl(thio)urea analogues by replacing the phenyl with a 2-pyridylgroup. The substituted guanidine variations proved to be almost inactive whereas the nitroethylene analogues appeared to be quite efficient. These results were interpreted in terms of the preferential cis-trans conformation of the aroyl(thio) urea and 2-pyridyl(thio)urea moieties involving the existence of hydrogen bonding. In vivo experiments showed that compound 7m had maximal antiamnestic activity at 0.03 mg/kg with a therapeutic ratio greater than 1000, while cholinergic sideeffects were only seen at doses 100-fold the maximally effective antiamnestic dose. Compound 7m represents a potentially interesting antidementia agent.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/08/20 alle ore 17:04:47