Yoo, Euna Hayat, Faisal Rhim, Hyewhon Choo, Hea-Young Park 2024-01-20T15:02:17Z 2024-01-20T15:02:17Z 2021-09-04 2012-04-15 0968-0896 https://pubs.kist.re.kr/handle/201004/129333 A series of novel N,N-dimethyl-N'-(5-(Ar-sulfonamido) benzo[d]isothiazol-3-yl)formimidamides was designed and synthesized as 5-HT6 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 Ca2+ increases (9b; IC50 = 0.36 mu M and 9i; IC50 = 0.44 mu M), indicating that 9b and 9i were potent 5-HT6 receptor antagonists. Compounds 9i also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors. (C) 2012 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD RAT LOCALIZATION CLONING AFFINITY LIGANDS POTENT Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists Article 10.1016/j.bmc.2012.02.020 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.20, no.8, pp.2707 - 2712 BIOORGANIC & MEDICINAL CHEMISTRY 20 8 2707 2712 scie scopus 000302767100028 2-s2.0-84859428852 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article RAT LOCALIZATION CLONING AFFINITY LIGANDS POTENT 5-HT6 receptor antagonists Benzoisothiazole Sulfonamide N,N-dimethylformimidamide