title: 3-Substituted, 3-(4-pyridinylmethyl)-1,3-dihydro-1-phenyl-2H-indol-2-ones as acetylcholine release enhancers: synthesis and SAR.
abstract: A series of 3-substituted, 3-(4-pyridinylmethyl)-1,3-dihydro-1-phenyl-2H-indol-2-ones was synthesized and found to enhance the stimulus-induced release of neurotransmitter acetylcholine (AcCh), and by doing so, might be useful in treating cognitive disorders where the level of this neurotransmitter may be diminished in the brain, as in Alzheimer's disease. An attempt has been made to correlate the structure of the 3-substitution with the ability of the compounds to enhance the release of AcCh from the striatum region of rat brain preparations.
authors.affiliation: Du Pont Merck Pharmaceutical Company, Wilmington, Delaware 19880-0353.
authors.forename: W W
authors.initials: WW
authors.lastname: Wilkerson
authors.forename: A A
authors.initials: AA
authors.lastname: Kergaye
authors.forename: S W
authors.initials: SW
authors.lastname: Tam
mesh_terms: D000109:Acetylcholine / Q000378:metabolism*; D000544:Alzheimer Disease / Q000188:drug therapy; D000647:Amnesia / Q000209:etiology / Q000503:physiopathology; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects / Q000502:physiology; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D000860:Hypoxia; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D011725:Pyridines; C083594:2,3-dihydro-2-oxo-1-phenyl-3-(4-pyridinylmethyl)-1H-indole-3-butanoic acid ethyl ester; C083595:2,3-dihydro-2-oxo 1-phenyl-3-(4-pyridinylmethyl)-1H-indole-3-pentanenitrile; C061017:linopirdine; D000109:Acetylcholine