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Design,synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists |
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| Authors: | Shilan Liu Yinhui Liu Hongmei Wang YiLi Ding Hao Wu Jingchao Dong Angela Wong Shu-Hui Chen Ge Li Manuel Chan Nicole Sawyer Francois G Gervais Martin Henault Stacia Kargman Leanne L Bedard Yongxin Han Rick Friesen Robert B Lobell David M Stout |
| Institution: | 1. WuXi PharmaTech Co. Ltd, 288 FuTe Zhong Road, No. 1 Building, WaiGaoQiao Free Trade Zone, Shanghai 200131, PR China;2. Department of Medicinal Chemistry, Merck Frosst Center for Therapeutic Research, Merck-Frosst Canada Ltd, PO Box 1005, Pointe Claire-Dorval, Quebec, Canada H9R 4P8;3. Department of Biochemistry and Molecular Biology, Merck Frosst Center for Therapeutic Research, Merck-Frosst Canada Ltd, PO Box 1005, Pointe Claire-Dorval, Quebec, Canada H9R 4P8;4. Merck Research Laboratories, West Point, PA 19486, USA;5. Merck Research Laboratories, Rahway, NJ 07065, USA |
| Abstract: | We describe herein a novel series of 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective inhibitors against the CXCR2 chemokine receptor and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Furthermore, these alkyl-hydrazine series inhibitors such as 5b demonstrated acceptable metabolic stability when incubated in human and rat microsomes. |
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