Schizophrenia is a debilitating disorder that affects nearly 1% of the global population. For the goal of controlling symptoms, several new treatments are available for initial and maintenance therapy. However, most of the treatments cause a plethora of side effects. Thus, there is an un-met medical need for a therapy which alleviates neuropsychiatric symptoms with no or minimal side effects. A series of 1,2,4-triazine-3-one derivatives were designed synthesized and evaluated for their in vitro potencies towards 5-HT2A, 5-HT1A receptors, dopamine receptor D2 and serotonin transporter (SERT). Most of the compounds showed potent in vitro potencies towards the selected receptors. The selected compounds were evaluated for their pharmacokinetic properties to assess bio-availability, exposures in plasma and brain. Details of design, chemistry, structure activity relationship, in vitro potencies, pharmacokinetic studies and in vivo efficacy of 1,2,4-triazine-3-one derivatives will be disclosed in this poster presentation.

Novel 1,2,4-triazine-3-one derivatives as multimodal compounds for the treatment of schizophrenia

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.