Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists

Bioorg Med Chem Lett. 2011 Jan 1;21(1):346-9. doi: 10.1016/j.bmcl.2010.11.001.

Ramakrishna V S Nirogi ¹, Amol D Deshpande, Ramasastri Kambhampati, Rajesh Kumar Badange, Laxman Kota, Anand V Daulatabad, Anil K Shinde, Ishtiyaque Ahmad, Vishwottam Kandikere, Pradeep Jayarajan, P K Dubey

Affiliations

Affiliation

1 Discovery Research, Medicinal Chemistry, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India. [email protected]

PMID: 21134749 DOI: 10.1016/j.bmcl.2010.11.001

Abstract

N(1)-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT(6) receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT(6) receptor. The compound 7a (K(i) = 3.4 nM, functional assay IC(50) = 310 nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter.

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