91849-57-9Relevant academic research and scientific papers
3-substituted coumarin derivatives and their use
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Paragraph 0088; 0089; 0090; 0107; 0108, (2016/10/08)
The invention provides a 3-substituted coumarin derivative, and pharmaceutically acceptable salts, solvates, hydrates or crystal forms thereof. The above compound has a high calcium flow activity and a very good selectivity on a human derived cannabinoid receptor CB2, and is a specific agonist or inverse agonist of the cannabinoid receptor CB2. The compound is an active ligand of a novel cannabinoid II receptor CB2, and compounds of the above kind and pharmaceutically acceptable salts, solvates, hydrates or crystal forms thereof have high calcium flow activities and a very good selectivity on the human derived cannabinoid receptor CB2. The compound is the specific agonist or inverse agonist of the cannabinoid receptor CB2, and can be applied to the preparation of medicines for treating, preventing and inhibiting CB2 receptor mediated diseases. The structure of the derivative is represented by a general formula A shown in the specification.
Design, syntheses, structure - Activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor
Han, Shuang,Zhang, Fei-Fei,Qian, Hai-Yan,Chen, Li-Li,Pu, Jian-Bin,Xie, Xin,Chen, Jian-Zhong
, p. 16 - 32 (2015/03/05)
The CB2 receptor has been considered as an inspiring drug target for the treatment of pain and immune-related diseases. In the current manuscript, a novel series of coumarin derivatives is reported to be designed and synthesized by combining the structural features of some known ligands for the cannabinoid receptors based on the CoMFA model of the lead compounds. The compounds were evaluated to be highly selective ligands for the CB2 receptor over the CB1 receptor by calcium mobilization assays. Furthermore, SAR results Therefore, molecular docking simulations were performed to calculate the receptor-ligand interactions of our synthesized compounds binding to the CB2 receptor. The understanding of the binding modes could be advantageous for further development of selective ligands for the CB2 receptor.
