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Novel bisstyryl derivatives of bakuchiol: targeting oral cavity pathogens
Mallepally V Reddy1, Niranjan Thota, Payare L Sangwan
1Department of Bioorganic Chemistry, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180001, India.
Abstract:
Novel bisstyryl derivatives of bakuchiol using Heck coupling reaction as the key step were synthesized and screened against a panel of six oral cavity pathogens for their antimicrobial activity. Four compounds (9-12) showed two to fourfold and four to eightfold better activity (MIC 0.25-16 microg/ml) than bakuchiol and triclosan respectively. These compounds effectively inhibit the biofilm formation of single and multiple species at 2 - 8 x MICs. 4- and 4'-Hydroxy/methoxy styryl moieties of the bakuchiol derivatives play a pivotal role towards the activity as established in the SAR studies. Mechanism of action studies revealed microbial membrane structure disruption as the probable mode of action of these compounds.
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