强效 BLT2 激动剂作为潜在伤口愈合促进剂的首次结构-活性关系研究。
First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters.
机构信息
Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
Institute of Pharmaceutical Technology and Buchmann Institute for Molecular Life Sciences, Goethe University, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.
出版信息
J Med Chem. 2020 Oct 22;63(20):11548-11572. doi: 10.1021/acs.jmedchem.0c00588. Epub 2020 Oct 6.
The first potent leukotriene B4 (LTB4) receptor type 2 (BLT2) agonists, endogenous 12()-hydroxyheptadeca-5,8,10-trienoic acid (12-HHT), and synthetic CAY10583 (CAY) have been recently described to accelerate wound healing by enhanced keratinocyte migration and indirect stimulation of fibroblast activity in diabetic rats. CAY represents a very valuable starting point for the development of novel wound-healing promoters. In this work, the first structure-activity relationship study for CAY scaffold-based BLT2 agonists is presented. The newly prepared derivatives showed promising wound-healing activity.
新型强效白三烯 B4（LTB4）受体 2（BLT2）激动剂，内源性 12（）-羟基十七碳-5,8,10-三烯酸（12-HHT）和合成的 CAY10583（CAY），最近被描述为通过增强糖尿病大鼠角质细胞迁移和间接刺激成纤维细胞活性来加速伤口愈合。CAY 为新型伤口愈合促进剂的开发提供了一个非常有价值的起点。在这项工作中，首次对基于 CAY 支架的 BLT2 激动剂进行了构效关系研究。新制备的衍生物显示出有前景的伤口愈合活性。
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