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Kava analogues as agents for treatment of periodontal diseases: Synthesis and initial biological evaluation
Authors:Bin Cai  James S Panek  Salomon Amar
Institution:1. Department of Chemistry, Boston University, Metcalf Center for Science and Engineering, 590 Commonwealth Avenue, Boston, MA 02215, United States;2. Department of Pharmacology, New York Medical College, Valhalla, NY, United States
Abstract: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 α,β-unsaturated ketone show promise in the prevention and treatment of inflammation and alveolar bone loss associated with periodontitis.
Keywords:Kava  Periodontal disease  Cyclohexene benzoate  Buchwald coupling
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