Analogues of the potential antipsychotic agent 1192U90: amide modifications

F Navas III, FLM Tang, LT Schaller…

Index: Navas III, Frank; Tang, Flora L. M.; Schaller, Lee T.; Norman, Mark H. Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 6 p. 811 - 823

Full Text: HTML

Citation Number: 8

Abstract

Analogues of 2-amino-N-(4-(4-(1, 2-benzisothiazol-3-yl)-1-piperazinyl)-butyl) benzamide hydrochloride (1192U90) were prepared and evaluated in receptor binding assays for the dopamine D2, serotonin 5-HT1a, and serotonin 5-HT2 receptors. Eight compounds have been synthesized in which the amide group of 1192U90 has been replaced with a variety of functional groups (ie ester, ketone, thioamide, butyramide, butyranilide, sulfonamide, ...