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Titolo:
Synthesis and structure-activity relationships in a set of new antimuscarinic agents
Autore:
De Amici, M; Conti, P; Vistoli, G; Carrea, G; Ottolina, G; De Micheli, C;
Indirizzi:
Univ Milan, Ist Chim Farmaceut & Tossicol, I-20131 Milan, Italy Univ Milan Milan Italy I-20131 armaceut & Tossicol, I-20131 Milan, Italy CNR, Ist Biocatalisi & Riconoscimento Mol, I-20131 Milan, Italy CNR Milan Italy I-20131 alisi & Riconoscimento Mol, I-20131 Milan, Italy
Titolo Testata:
MEDICINAL CHEMISTRY RESEARCH
fascicolo: 9, volume: 10, anno: 2001,
pagine: 615 - 633
SICI:
1054-2523(2001)10:9<615:SASRIA>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
M-3 RECEPTOR ANTAGONIST; ACETYLCHOLINE-RECEPTORS; MUSCARINIC RECEPTORS; BIOLOGICAL-ACTIVITY; HIGH SELECTIVITY; PHARMACOLOGY; DERIVATIVES; ENANTIOMERS; ISOXAZOLES; MUSCARONE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: De Micheli, C Univ Milan, Ist Chim Farmaceut & Tossicol, Vle Abruzzi 42, I-20131 Milan, Italy Univ Milan Vle Abruzzi 42 Milan Italy I-20131 Milan, Italy
Citazione:
M. De Amici et al., "Synthesis and structure-activity relationships in a set of new antimuscarinic agents", MED CHEM RE, 10(9), 2001, pp. 615-633

Abstract

Three quaternary ammonium salts (4-6), related to muscarine and muscarone,were designed as antimusearinic agents and synthesized by means of a iodoetherification reaction carried out on an unsaturated diol. The structurallyrelated furanone 7 together with isoxazoles 10-12 and Delta (2)-isoxazolines 14 and 15 were in turn obtained via 1,3-dipolar cyloaddition of benzoylformonitrile oxide to suitable alkynes and alkenes. The new derivatives weretested in vitro for antimuscarinic activity at guinea pig atria (M-2) and at two different M-3 tissue preparations (rat jejunum and guinea pig bladder). Selected compounds were also examined for binding activity at M-1, M-2,and M-3 muscarinic receptors. The major part of the derivatives under study behaved as highly potent, though non selective, muscarinic antagonists. We propose selected geometrical parameters capable of predicting the selectivity of new antagonists for M-2 versus M-3 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 08:16:55