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First Structure–Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters

Authors :
Viktoria Planz
Victor Hernandez-Olmos
Ting Liu
Dieter Steinhilber
Alexander Kaps
Rinusha Rajkumar
Ewgenij Proschak
Maike Windbergs
Jan Heering
Astrid Kaiser
Michael J. Parnham
Matthias Gramzow
Manfred Schubert-Zsilavecz
Source :
Journal of Medicinal Chemistry. 63:11548-11572
Publication Year :
2020
Publisher :
American Chemical Society (ACS), 2020.

Abstract

The first potent leukotriene B4 (LTB4) receptor type 2 (BLT2) agonists, endogenous 12(S)-hydroxyheptadeca-5Z,8E,10E-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 in vitro wound-healing activity.

Details

ISSN :
15204804 and 00222623
Volume :
63
Database :
OpenAIRE
Journal :
Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....a476826fd6488d69a4334821d320f448
Full Text :
https://doi.org/10.1021/acs.jmedchem.0c00588