Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: A novel series of atypical antipsychotic agents

…, SY Kim, WK Park, JH Choi, CM Seong

Index: Park, Chul Min; Kim, So Young; Park, Woo Kyu; Choi, Jung Hwan; Seong, Churl Min Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5221 - 5224

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Citation Number: 5

Abstract

(Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT2C and 5-HT6 receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin-1-yl)-phenyl]-amide (6b) exhibits the highest affinity towards both 5-HT2C (IC50= 4nM) and 5-HT6 receptors (IC50= 3nM) with good selectivity over other serotonin (5-HT1A, 5-HT2A, and 5-HT7) and dopamine (D2–D4) receptor ...