|
|||||
|
|
Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists |
|
| Authors: | 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 P K |
| Institution: | a Discovery Research - Medicinal Chemistry, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India b Discovery Research - In-vitro Biology, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India c Discovery Research - Drug Metabolism and Phamacokinetics, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India d Discovery Research - In-vivo Biology, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India e Department of Chemistry, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad 500 085, India |
| 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 = 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. |
| Keywords: | 5-HT6 receptor ligands Antagonists Cognition PK profile |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |