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

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

N sub(1)-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT sub(6) receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT sub(6) receptor. The compound 7a (K sub(i) = 3.4 nM, functional assay IC sub(50) = 310 nM)...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.346-349
Hauptverfasser: Nirogi, Ramakrishna VS, Deshpande, Amol D, Kambhampati, Ramasastri, Badange, Rajesh Kumar, Kota, Laxman, Daulatabad, Anand V, Shinde, Anil K, Ahmad, Ishtiyaque, Kandikere, Vishwottam, Jayarajan, Pradeep, Dubey, P K
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Sprache:eng
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Zusammenfassung:N sub(1)-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT sub(6) receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT sub(6) receptor. The compound 7a (K sub(i) = 3.4 nM, functional assay IC sub(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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.11.001