Kava Analogues as Agents for Treatment of Periodontal Diseases: Synthesis and Initial Biological Evaluation
Six kava analogues of the structural type 3-oxocyclohex-1-en-1-yl benzoates (and corresponding benzamides) were synthesized and evaluated for their affect on periodontal deconstruction in collagen anti-body primed oral gavage model of periodontitis. The compounds were prepared through an acylation or amidation of the enolizable cyclic 1,3-diketone. We have learned that three of the analogues are responsible for the reduction of inflammatory cell counts within soft tissue. These novel kava-like molecules where the lactone is replaced by an alpha,beta-unsaturated ketone show promise in the prevention and treatment of inflammation and alveolar bone loss associated with periodontitis.
Cai, B., Panek, J., & Amar, S. (2018). Kava Analogues as Agents for Treatment of Periodontal Diseases: Synthesis and Initial Biological Evaluation. Bioorganic & Medicinal Chemistry Letters, 28 (16), 2667-2669. https://doi.org/10.1016/j.bmcl.2018.05.026