Synthesis and biological activity of the putative metabolites of the atypical antipsychotic agent tiospirone

JA Cipollina, EH Ruediger, JS New…

Index: Cipollina, Joseph A.; Ruediger, Edward H.; New, James S.; Wire, Mary E.; Shepherd, Timothy A.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 11 p. 3316 - 3328

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Citation Number: 33

Abstract

Putative oxidative metabolites of the lead antipsychotic agent tiospirone (1) were synthesized to assist in the identification of the authentic metabolic products found in human urine samples. Thus far, six authentic metabolites have been correlated to the synthetic species.'. The putative metabolites were further examined in vitro to assess their central nervous system therapeutic potential. SAR analysis of these derivatives indicates that ...