학술논문
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity
Document Type
Article
Author
Source
Subject
*SEROTONIN agonists
*OBESITY treatment
*DRUG design
*PIPERAZINE
*DOSE-effect relationship in pharmacology
*ORAL drug administration
*INGESTION
*MEDICAL model
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Language
ISSN
0960-894X
Abstract
Abstract: Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure–activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose–responsive in vivo efficacy in our pre-clinical food intake model. [Copyright &y& Elsevier]