期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 8, 页码 2684-2690出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.018
关键词
EP1 antagonist; pain; conformational constraint; scaffold hopping; lead hopping
We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain. (C) 2008 Elsevier Ltd. All rights reserved.
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