Indole-3-piperazinyl derivatives: Novel chemical class of 5-HT 6 receptor antagonists

…, AK Shinde, I Ahmad, V Kandikere, P Jayarajan…

Index: Nirogi, Ramakrishna V.S.; Deshpande, Amol D.; Kambhampati, Ramasastri; Badange, Rajesh Kumar; Kota, Laxman; Daulatabad, Anand V.; Shinde, Anil K.; Ahmad, Ishtiyaque; Kandikere, Vishwottam; Jayarajan, Pradeep; Dubey Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 346 - 349

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Citation Number: 16

Abstract

N1-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT6 receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT6 receptor. The compound 7a (Ki= 3.4 nM, functional assay IC50= 310nM) 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 ...