DSpace at EWHA: Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT 6 receptor antagonists

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DC Field	Value	Language
dc.contributor.author	박혜영	-
dc.date.accessioned	2016-08-28T12:08:13Z	-
dc.date.available	2016-08-28T12:08:13Z	-
dc.date.issued	2012	-
dc.identifier.issn	0968-0896	-
dc.identifier.other	OAK-8667	-
dc.identifier.uri	https://dspace.ewha.ac.kr/handle/2015.oak/222547	-
dc.description.abstract	A series of novel N,N-dimethyl-N′-(5-(Ar-sulfonamido) benzo[d]isothiazol-3-yl)formimidamides was designed and synthesized as 5-HT 6 ligands. Here N,N-dimethyl formimidamides was used as a replacement for an aminoethyl moiety. In vitro functional assays demonstrated compounds 9b and 9i significantly inhibited the 5-HT-induced Ca 2+ increases (9b; IC 50 = 0.36 μM and 9i; IC 50 = 0.44 μM), indicating that 9b and 9i were potent 5-HT 6 receptor antagonists. Compounds 9i also showed good selectivity on the 5-HT 6 over 5-HT 4 and 5-HT 7 receptors. © 2012 Published by Elsevier Ltd. All rights reserved.	-
dc.language	English	-
dc.title	Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT 6 receptor antagonists	-
dc.type	Article	-
dc.relation.issue	8	-
dc.relation.volume	20	-
dc.relation.index	SCI	-
dc.relation.index	SCIE	-
dc.relation.index	SCOPUS	-
dc.relation.startpage	2707	-
dc.relation.lastpage	2712	-
dc.relation.journaltitle	Bioorganic and Medicinal Chemistry	-
dc.identifier.doi	10.1016/j.bmc.2012.02.020	-
dc.identifier.wosid	WOS:000302767100028	-
dc.identifier.scopusid	2-s2.0-84859428852	-
dc.author.google	Yoo E.	-
dc.author.google	Hayat F.	-
dc.author.google	Rhim H.	-
dc.author.google	Park Choo H.-Y.	-
dc.contributor.scopusid	박혜영(34972649500;57200273796)	-
dc.date.modifydate	20230411110509	-