100325-47-1Relevant articles and documents
IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page/Page column 34-35, (2010/02/07)
A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Design, synthesis, and SAR of tachykinin antagonists: Modulation of balance in NK1/NK2 receptor antagonist activity
Albert, Jeffrey S.,Andisik, Donald,Barthlow, Herbert,Bernstein, Peter R.,Bialecki, Russell A.,Dedinas, Robert,Dembofsky, Bruce T.,Hill, Daniel,Kirkland, Karin,Koether, Gerard M.,Kosmider, Benedict J.,Ohnmacht, Cyrus,Palmer, William,Potts, William,Rumsey, William,Shen, Lihong,Shenvi, Ashok,Sherwood, Scott,Aharony, David,Warwick, Paul J.,Russell, Keith
, p. 3972 - 3983 (2007/10/03)
Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was found that alteration of two key regions could modulate the balance of NK1 and NK2 potency. Substitution of the 2-naphthalene position in analogues of ZD6021 resulted in increased NK1 potency and thus afforded NK1 preferential antagonists. Alterations of the piperidine region could then increase NK2 potency to restore dual NK1/NK2 selectivity. Through these efforts, three novel receptor antagonists from a single chemically related series were identified; two are dual NK1/NK2 antagonists, and the third is an NK1 preferential antagonist. In this paper, the factors affecting the balance of NK1 and NK2 selectivity in this series are discussed and the in vitro and in vivo properties of the novel antagonists are described.
7-heterocyclic-1,4-dihydroquinolones
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, (2008/06/13)
1-Alkyl-6,8-difluoro-7-heterocyclic-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by conventional cyclization methods.