Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands |
| |
| Authors: | Nirogia Ramakrishna V S Kambhampati Ramasastri Daulatabad Anand V Gudla Parandhama Shaikh Mohammad Achanta Pramod Kumar Shinde Anil K Dubey Pramod Kumar |
| |
| Affiliation: | Discovery Research-Medicinal Chemistry, Suven Life Sciences Ltd, Serene Chambers, Banjara Hills, Hyderabad, India. ramakrishna_nirogi@yahoo.co.in |
| |
| Abstract: | A series of novel conformationally restricted N(1)-arylsulfonyl-3-aminoalkoxy indoles were designed and synthesized as 5-HT(6) receptor (5-HT(6)R) ligands. Many of the synthesized compounds have moderate in vitro-binding affinities at 5-HT(6)R. The lead compound 8b (% inhibition?=?97.2 at 1 μM) from this series has good pharmacokinetic profile in male Wister rats and is active in animal model of cognition like Morris water maze. The details of chemistry, SAR, pharmacokinetics and pharmacological data constitute the subject matter of this report. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
