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Titolo:
Agonists at the alpha 4 beta 2 nicotinic acetylcholine receptors: Structure-activity relationships and molecular modelling
Autore:
Tonder, JE; Olesen, PH;
Indirizzi:
Novo Nordisk AS, Hlth Care Discovery, DK-2760 Malov, Denmark Novo Nordisk AS Malov Denmark DK-2760 Discovery, DK-2760 Malov, Denmark
Titolo Testata:
CURRENT MEDICINAL CHEMISTRY
fascicolo: 6, volume: 8, anno: 2001,
pagine: 651 - 674
SICI:
0929-8673(200105)8:6<651:AATA4B>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHOLINERGIC CHANNEL ACTIVATOR; PYRROLIDINE-MODIFIED ANALOGS; MPTP-TREATED MONKEYS; BIOLOGICAL EVALUATION; ALZHEIMERS-DISEASE; HIGH-AFFINITY; IN-VITRO; BINDING; PHARMACOLOGY; EPIBATIDINE;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
86
Recensione:
Indirizzi per estratti:
Indirizzo: Olesen, PH Novo Nordisk AS, Hlth Care Discovery, Novo Nordisk Pk, DK-2760 Malov, Denmark Novo Nordisk AS Novo Nordisk Pk Malov Denmark DK-2760 Denmark
Citazione:
J.E. Tonder e P.H. Olesen, "Agonists at the alpha 4 beta 2 nicotinic acetylcholine receptors: Structure-activity relationships and molecular modelling", CURR MED CH, 8(6), 2001, pp. 651-674

Abstract

Agonists of the alpha4 beta2 nicotinic acetylcholine receptors have been synthesised as potential drugs for treatment of a variety of diseases. In this review, the published nicotinic agonists are presented and, on the basisof the molecular structure, the compounds are divided into three compound classes, nicotinoids (structurally close to nicotine), bicyclic compounds (structurally close to epibatidine and anatoxin-a), and analogues of imidacloprid (structurally close to the insecticide imidacloprid). The structure-activity relationships are discussed within and in between the classes. On the basis of computational studies of ligands for the nicotinic acetylcholine receptors the structure-activity relationships are discussed and a possible binding mode suggested. The binding mode encompasses: (A) an interaction between an anionic site in the receptor and the protonated nitrogen atom in the ligand, (B) a hydrogen bond between a hydrogen bond donor in thereceptor and a hydrogen bond acceptor in the ligand, (C) an interaction between a pi -system (heteroaromatic ring, carbonyl bond) in the ligand and another pi -system or a positively charged amino acid residue in the bindingsite, (D) a pi -cation interaction between aromatic residues in the receptor binding site and the protonated nitrogen atom in the ligand, and (E) steric interactions of positive and negative character around the aliphatic and the heteroaromatic part of the ligand.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 07:26:51