N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II
| Title: | N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II |
|---|---|
| Authors: | Elliott, Jason M.; Carling, Robert W.; Chicchi, Gary G.; Crawforth, James; Hutson, Peter H.; Jones, A. Brian; Kelly, Sarah; Marwood, Rose; Meneses-Lorente, Georgina; Mezzogori, Elena; Murray, Fraser; Rigby, Michael; Royo, Inmaculada; Russell, Michael G N; Shaw, Duncan; Sohal, Bindi; Tsao, Kwei Lan; Williams, Brian |
| Source: | Elliott, J M, Carling, R W, Chicchi, G G, Crawforth, J, Hutson, P H, Jones, A B, Kelly, S, Marwood, R, Meneses-Lorente, G, Mezzogori, E, Murray, F, Rigby, M, Royo, I, Russell, M G N, Shaw, D, Sohal, B, Tsao, K L & Williams, B 2006, 'N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 22, pp. 5752-5756. https://doi.org/10.1016/j.bmcl.2006.08.085 |
| Publication Year: | 2006 |
| Collection: | The University of Manchester: Research Explorer - Publications |
| Subject Terms: | N′-2-Diphenylquinoline-4-carbohydrazide; NK3; Schizophrenia |
| Description: | Introduction of selected amine containing side chains into the 3-position of N′,2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwanted hIKr affinity and a piperazine N-tert-butyl group is necessary for metabolic stability. The lead compound (8m) occupies receptors within the CNS following oral dosing (Occ90 7 mg/kg po; plasma Occ90 0.4 μM) and has good selectivity and excellent PK properties. © 2006 Elsevier Ltd. All rights reserved. |
| Document Type: | article in journal/newspaper |
| Language: | English |
| ISSN: | 1464-3405 |
| Relation: | info:eu-repo/semantics/altIdentifier/pmid/16950617; info:eu-repo/semantics/altIdentifier/eissn/1464-3405 |
| DOI: | 10.1016/j.bmcl.2006.08.085 |
| Availability: | https://research.manchester.ac.uk/en/publications/a20b7226-25cd-406b-a241-6a213d98759e; https://doi.org/10.1016/j.bmcl.2006.08.085 |
| Rights: | info:eu-repo/semantics/closedAccess |
| Accession Number: | edsbas.FE31FF27 |
| Database: | BASE |