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

Title
Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT 6 receptor antagonists
Authors
Yoo E.Hayat F.Rhim H.Park Choo H.-Y.
Ewha Authors
박혜영
SCOPUS Author ID
박혜영scopus
Issue Date
2012
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 20, no. 8, pp. 2707 - 2712
Indexed
SCI; SCIE; SCOPUS WOS scopus
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.
DOI
10.1016/j.bmc.2012.02.020
Appears in Collections:
약학대학 > 약학과 > Journal papers
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