Synthesis and Structure Activity Relationship of Rigidized Indolyl Pyrrolidine Derivatives as 5-HT6 Receptor Ligands

Ramakrishna Nirogi; Adireddy Dwarampudi; Venugopalarao Bhatta; Laxman Kota; P.K. Dubey

doi:10.14233/ajchem.2013.15443

Issue

Vol. 25 No. 16 (2013): Vol 25 Issue 16

Issue Published : 9 October 2013

This work is licensed under a Creative Commons Attribution 4.0 International License.

Synthesis and Structure Activity Relationship of Rigidized Indolyl Pyrrolidine Derivatives as 5-HT6 Receptor Ligands

https://doi.org/10.14233/ajchem.2013.15443

Ramakrishna Nirogi

Discovery Research, Suven Life Sciences Ltd., Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad-500 034, India

Adireddy Dwarampudi

Discovery Research, Suven Life Sciences Ltd., Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad-500 034, India ; Department of Chemistry, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad-500 085, India

Venugopalarao Bhatta

Discovery Research, Suven Life Sciences Ltd., Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad-500 034, India

Laxman Kota

Discovery Research, Suven Life Sciences Ltd., Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad-500 034, India

P.K. Dubey

Department of Chemistry, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad-500 085, India

Corresponding Author(s) : Ramakrishna Nirogi

nvsrk@suven.com

Asian Journal of Chemistry, Vol. 25 No. 16 (2013): Vol 25 Issue 16
Article Published : 9 October 2013

Abstract

A novel series of rigidized indolyl pyrrolidine derivatives have been designed by constraining the tryptamine nitrogen through a and b carbons. All the synthesized derivatives have shown moderate affinities at 5-HT₆R when tested in in vitro binding assay. Synthesis, structure activity relationship (SAR), pharmacokinetic profile and in vivo efficacy of a selected compound is the subject matter of this communication.

Keywords

5-HT6R Structure activity relationship Pharmacokinetic Brain penetration Water maze Cognition

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Nirogi, R.; Dwarampudi, A.; Bhatta, V.; Kota, L.; Dubey, P. Synthesis and Structure Activity Relationship of Rigidized Indolyl Pyrrolidine Derivatives As 5-HT6 Receptor Ligands. ajc 2013, 25, 9293-9298.