Abstract
A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability. Following various strategies, compounds with a good stability in liver microsomes and rat PK profile have been identified. © 2011 Elsevier Ltd. All rights reserved.
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Riether, D., Wu, L., Cirillo, P. F., Berry, A., Walker, E. R., Ermann, M., … Thomson, D. S. (2011). 1,4-Diazepane compounds as potent and selective CB2 agonists: Optimization of metabolic stability. Bioorganic and Medicinal Chemistry Letters, 21(7), 2011–2016. https://doi.org/10.1016/j.bmcl.2011.02.017
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