✦ LIBER ✦

Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists

✍ Scribed by Martin Pettersson; Brian M. Campbell; Amy B. Dounay; David L. Gray; Longfei Xie; Christopher J. O’Donnell; Nancy C. Stratman; Kim Zoski; Elena Drummond; Gary Bora; Al Probert; Tammy Whisman

Book ID: 104005136
Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 718 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.11.066

No coin nor oath required. For personal study only.

✦ Synopsis

Compounds with combined norepinephrine reuptake inhibitor (NRI) and serotonin 1A (5-HT 1A ) partial agonist pharmacology may offer a new therapeutic approach for treating symptoms of neuropsychiatric disorders including ADHD, depression, and anxiety. Herein we describe the design and optimization of novel chemical matter that exhibits favorable dual NRI and 5-HT 1A partial agonist activity. Lead compounds in this series were found to be devoid of activity at the dopamine transporter and were shown to be brain penetrant with high receptor occupancy.

📜 SIMILAR VOLUMES

ChemInform Abstract: Design, Synthesis,

ChemInform Abstract: Design, Synthesis, and Pharmacological Evaluation of Azetedine and Pyrrolidine Derivatives as Dual Norepinephrine Reuptake Inhibitors and 5-HT1A Partial Agonists.

✍ Martin Pettersson; et al. et al. 📂 Article 📅 2011 🏛 John Wiley and Sons ⚖ 34 KB 👁 2 views

Synthesis and Structure−Activity Relatio

Synthesis and Structure−Activity Relationship in a Class of Indolebutylpiperazines as Dual 5-HT1A Receptor Agonists and Serotonin Reuptake Inhibitors

✍ Heinrich, Timo; Böttcher, Henning; Gericke, Rolf; Bartoszyk, Gerd D.; Anzali, So 📂 Article 📅 2004 🏛 American Chemical Society 🌐 English ⚖ 204 KB

Synthesis, Potency, and in Vivo Evaluati

Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT 1A Receptor Antagonists

✍ Zhou, Dahui; Stack, Gary P.; Lo, Jennifer; Failli, Amedeo A.; Evrard, Deborah A. 📂 Article 📅 2009 🏛 American Chemical Society 🌐 English ⚖ 874 KB

De novo design, synthesis and pharmacolo

De novo design, synthesis and pharmacological evaluation of new azaindole derivatives as dual inhibitors of Abl and Src kinases

✍ Chevé, Gwénaël; Bories, Cédric; Fauvel, Bénédicte; Picot, François; Tible, Alix; 📂 Article 📅 2012 🏛 The Royal Society of Chemistry 🌐 English ⚖ 450 KB

Synthesis and Evaluation of a Novel Seri

Synthesis and Evaluation of a Novel Series of Pyrrolizine Derivatives as Dual Cyclooxygenase-1 and 5-Lipoxygenase Inhibitors

✍ Stefan Laufer; Hans-Günter Striegel; Karola Neher; Pia Zechmeister; Cornelia Don 📂 Article 📅 1997 🏛 John Wiley and Sons 🌐 English ⚖ 625 KB

Design, synthesis and pharmacological ev

Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands

✍ Nirogi, Ramakrishna V.S.; Badange, Rajeshkumar; Kambhampati, Ramasastri; Chindhe 📂 Article 📅 2012 🏛 Elsevier Science 🌐 English ⚖ 445 KB