## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3
✍ Scribed by Steven M. Bromidge; Roberto Arban; Barbara Bertani; Manuela Borriello; Anna-Maria Capelli; Romano Di-Fabio; Stefania Faedo; Massimo Gianotti; Laurie J. Gordon; Enrica Granci; Alessandra Pasquarello; Simone K. Spada; Angela Worby; Laura Zonzini; Valeria Zucchelli
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 642 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT 1 autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of profiles at targets known to play a key role in the control of synaptic 5-HT levels will allow exploration of different pharmacological profiles in a range of animal behavioral and disease models.
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## Abstract Two benzodiazepines, Diazepam and Flunitrazepam, labeled with carbon‐14 in position 5 of the diazepine ring have been synthesized. Use of a condensation between iminochlorides and ^14^C‐benzonitriles, followed by exhaustive methylation of the resulting quinazolines and hydrolyses is des
## Abstract magnified image One‐pot reaction of 3‐aryl‐5‐methyl‐1,3,4‐oxadiazolin‐2‐ones **1a‐g** with ethanolamine yielded the 4‐(2‐hydroxyethyl)‐2‐aryl‐5‐methyl‐2,4‐dihydro‐3__H__‐1,2,4‐triazolin‐3‐ones **2a‐g** which were converted to the azido compounds **6a‐g**. These azides on 1,3‐dipolar cy