Abstract
Based on the previously reported discovery lead, 3-( cis-4-(4-(1 H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1 H-indole ( 2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT 1A receptor antagonists. The investigation of the structure–activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study, 5-(piperazin-1-yl)quinoline analog ( trans- 20), exhibited equal binding affinities at 5-HT transporter ( K i = 4.9 nM), 5-HT 1A receptor ( K i = 6.2 nM) and functioned as a 5-HT 1A receptor antagonist.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.