Novel atypical antipsychotic agents: Rational design, an efficient palladium-catalyzed route, and pharmacological studies

Giuseppe Campiani, Stefania Butini, Caterina Fattorusso, Francesco Trotta, Sandra Gemma, Bruno Catalanotti, Vito Nacci, Isabella Fiorini, Alfredo Cagnotto, Ilario Mereghetti, Tiziana Mennini, Patrizia Minetti, M. Assunta Di Cesare, M. Antonietta Stasi, Stefano Di Serio, Orlando Ghirardi, Ornella Tinti, Paolo Carminati

Research output: Contribution to journalArticlepeer-review

Abstract

Using rational drug design to develop atypical antipsychotic drug candidates, we generated novel and metabolically stable pyrrolobenzazepines with an optimized pKi 5-HT2A/O2 ratio. 5a, obtained by a new palladium-catalyzed three-step synthesis, was selected for further pharmacological and biochemical investigations and showed atypical antipsychotic properties in vivo. 5a was active on conditioned avoidance response at 0.56 mg/kg, it had low cataleptic potential and proved to be better than ST1899, clozapine, and olanzapine, representing a new clinical candidate.

Original languageEnglish
Pages (from-to)1705-1708
Number of pages4
JournalJournal of Medicinal Chemistry
Volume48
Issue number6
DOIs
Publication statusPublished - Mar 24 2005

ASJC Scopus subject areas

  • Organic Chemistry

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