NYMC Faculty Publications

Kava Analogues as Agents for Treatment of Periodontal Diseases: Synthesis and Initial Biological Evaluation

DOI

10.1016/j.bmcl.2018.05.026

Journal Title

Bioorganic & Medicinal Chemistry Letters

First Page

2667

Last Page

2669

Document Type

Article

Publication Date

September 2018

Department

Pharmacology

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 alpha,beta-unsaturated ketone show promise in the prevention and treatment of inflammation and alveolar bone loss associated with periodontitis.

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