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First Structure–Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters
- 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.
- Subjects :
- Keratinocytes
Cell Survival
Leukotriene B4
Receptors, Leukotriene B4
CHO Cells
Pharmacology
01 natural sciences
Structure-Activity Relationship
03 medical and health sciences
chemistry.chemical_compound
Cricetulus
Drug Development
Drug Discovery
medicine
Animals
HaCaT Cells
Humans
Structure–activity relationship
Keratinocyte migration
Fibroblast
Receptor
030304 developmental biology
Wound Healing
0303 health sciences
Molecular Structure
Hep G2 Cells
In vitro
0104 chemical sciences
010404 medicinal & biomolecular chemistry
HaCaT
medicine.anatomical_structure
chemistry
Molecular Medicine
Wound healing
Subjects
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