Design, synthesis and biological evaluation of GPR55 agonists.
GPR55, a G protein-coupled receptor, is an attractive target to alleviate inflammatory and neuropathic pain and treat osteoporosis and cancer. Identifying a potent and selective ligand will aid to further establish the specific physiological roles and pharmacology of the receptor. Towards this goal, a targeted library of 22 compounds was synthesized in a modular fashion to obtain structure-activity relationship information. The general route consisted of coupling a variety of p-aminophenyl sulfonamides to isothiocyanates to form acylthioureas. For the synthesis of a known naphthyl ethyl alcohol motif, route modification led to a shorter and more efficient process. The 22 analogues were analyzed for their ability to serve as agonists at GPR55 and valuable information for both ends of the molecule was ascertained.
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- Thiourea
- Structure-Activity Relationship
- Receptors, G-Protein-Coupled
- Receptors, Cannabinoid
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Humans
- Drug Design
- Dose-Response Relationship, Drug
- 3405 Organic chemistry
Citation
Published In
DOI
EISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- Thiourea
- Structure-Activity Relationship
- Receptors, G-Protein-Coupled
- Receptors, Cannabinoid
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Humans
- Drug Design
- Dose-Response Relationship, Drug
- 3405 Organic chemistry