209481-70-9Relevant academic research and scientific papers
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: A novel series of atypical antipsychotic agents
Park, Chul Min,Kim, So Young,Park, Woo Kyu,Choi, Jung Hwan,Seong, Churl Min
supporting information; experimental part, p. 5221 - 5224 (2010/10/01)
(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 = 4 nM) and 5-HT6 receptors (IC50 = 3 nM) with good selectivity over other serotonin (5-HT1A, 5-HT 2A, and 5-HT7) and dopamine (D2-D4) receptor subtypes. In 5-HT2C and 5-HT6 receptor functional assays, this compound showed considerable antagonistic activity for both receptors.
Sulphonamide derivatives, process for their preparation, and their use as medicaments
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, (2008/06/13)
Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed. The present compounds are of formula (I) or a salt thereof: wherein: P isbenzothiophene, benzothiadiazole, quinoline, benzofuran or indole; A is a single bond, a C1-6alkylene or a C1-6alkenylene group; R1is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, nitro, amino, C1-6alkylamino or C1-6dialkylamino, cyano or R1is phenyl or naphthyl; n is 0, 1, 2, 3, 4, 5, or 6; R2is hydrogen, C1-6alkyl or aryl C1-6alkyl or R2is linked to R3to form a group (CH2)2or (CH2)3; R3is a group R5or together with R5forms a group (CH2)2O or (CH2)3O or R3is linked to R2to form a group (CH2)2or (CH2)3; R4is an N-piperazine ring optionally substituted by C1-6alkyl; and R5is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, nitro, trifluoromethyl, cyano or aryl.
