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

Victor Hernandez-OlmosJan HeeringViktoria PlanzTing LiuAlexander KapsRinusha RajkumarMatthias GramzowAstrid KaiserManfred Schubert-ZsilaveczMichael J ParnhamMaike WindbergsDieter SteinhilberEwgenij Proschak
Published in: Journal of medicinal chemistry (2020)
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.
Keyphrases
  • wound healing
  • structure activity relationship
  • diabetic rats
  • oxidative stress
  • climate change
  • human health
  • tissue engineering