Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists
| Autor: | Laxman Kota, Amol D. Deshpande, Shinde Anil Karbhari, Ramakrishna Nirogi, Ishtiyaque Ahmad, P. K. Dubey, Anand V. Daulatabad, Pradeep Jayarajan, Rajesh Kumar Badange, Ramasastri Kambhampati, Vishwottam Kandikere |
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| Rok vydání: | 2010 |
| Předmět: |
Male
Indoles Stereochemistry Clinical Biochemistry Pharmaceutical Science Morris water navigation task Administration Oral Biochemistry Chemical synthesis Piperazines Structure-Activity Relationship Drug Discovery Animals Humans Rats Wistar Receptor Molecular Biology 5-HT receptor Indole test Sulfonamides Ligand Chemistry Organic Chemistry Antagonist Rats Receptors Serotonin 5-HT6 receptor Microsomes Liver Molecular Medicine Serotonin Antagonists Protein Binding |
| Zdroj: | Bioorganicmedicinal chemistry letters. 21(1) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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