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Literature DB >> 18799310

Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.

Snahel D Patel¹, Wendy M Habeski, Hyunsuk Min, Jiansu Zhang, Robin Roof, Bradley Snyder, Gary Bora, Brian Campbell, Cheryl Li, Debra Hidayetoglu, Douglas S Johnson, Archana Chaudhry, Maura E Charlton, Natasha M Kablaoui.

Abstract

The discovery of the CNS-penetrant and selective alpha(2C) adrenergic receptor antagonist N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, 13 is described. Structure-activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other alpha(2)-AR subtypes.

Entities: Chemical Gene

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Year: 2008 PMID： 18799310 DOI： 10.1016/j.bmcl.2008.08.055

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

2 in total

Review 1. Therapeutic Potential of Selectively Targeting the α_2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective.

Authors: Madeleine Monique Uys; Mohammed Shahid; Brian Herbert Harvey
Journal: Front Psychiatry Date: 2017-08-14 Impact factor: 4.157

2. A versatile catalyst system for enantioselective synthesis of 2-substituted 1,4-benzodioxanes.

Authors: Eugene Chong; Bo Qu; Yongda Zhang; Zachary P Cannone; Joyce C Leung; Sergei Tcyrulnikov; Khoa D Nguyen; Nizar Haddad; Soumik Biswas; Xiaowen Hou; Katarzyna Kaczanowska; Michał Chwalba; Andrzej Tracz; Stefan Czarnocki; Jinhua J Song; Marisa C Kozlowski; Chris H Senanayake
Journal: Chem Sci Date: 2019-03-13 Impact factor: 9.825

2 in total

Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.

Review 1. Therapeutic Potential of Selectively Targeting the α2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective.

2. A versatile catalyst system for enantioselective synthesis of 2-substituted 1,4-benzodioxanes.

Review 1. Therapeutic Potential of Selectively Targeting the α_2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective.