Methods: In terms of inhibitor design, a small molecule “click chemistry” strategy was employed whereby the azide-bearing partner constitutes a trisubstituted oxazole framework and the terminal acetylene partner constitutes a 1, 3-diaminotriazine framework.
Results: The design, synthesis and chemistry of the coupling partners in both the acetylenic and azido series have been accomplished. Four azido compounds have been synthesized and one acetylenic compound. The backbone structure of the acetylenic compound was tested for inhibition of P. gingivalis adherence to streptococci and was shown to block adherence by 25% and 67% at concentrations of 25µM and 50µM, respectively.
Conclusions: Bio-active small molecule peptidomimetics were synthesized that may represent therapeutic agents that could reduce P. gingivalis colonization of the oral cavity.
Keywords: Adherence and colonization, Biofilm, Microbiology, Periodontal organisms and Therapeutics