Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372785 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A high throughput screening campaign identified aryl 1,4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-like parameters as well as low microsomal stability and poor solubility. Structure–activity relationships are described with a focus on improving the drug-like parameters resulting in compounds with improved solubility and permeability.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Renée Zindell, Edward R. Walker, John Scott, Patricia Amouzegh, Lifen Wu, Monika Ermann, David Thomson, Micheal B. Fisher, Cody Lee Fullenwider, Heather Grbic, Paul Kaplita, Brian Linehan, Mita Patel, Monica Patel, Sabine Löbbe, Svenja Block,