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Novel bisstyryl derivatives of bakuchiol: Targeting oral cavity pathogens

IR@IIIM: CSIR-Indian Institute of Integrative Medicine, Jammu

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Title Novel bisstyryl derivatives of bakuchiol: Targeting oral cavity pathogens
 
Creator Reddy, Mallepally V.
Thota, Niranjan
Sangwan, Payare L.
Malhotra, Pankaj
Ali, Furqan
Khan, Inshad A.
Chimni, Swapandeep S.
Koul, Surrinder
 
Subject Chemical Sciences
 
Description 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 (9e12) showed two to fourfold and four to eightfold better activity (MIC 0.25e16 mg/ml)than bakuchiol and triclosan respectively. These compounds effectively inhibit the biofilm formation of single and multiple species at 2 e 8 � MICs. 4- and 40-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.
 
Date 2010
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://iiim.csircentral.net/300/1/10.1016j.ejmech.2010.03.049.pdf
Reddy, Mallepally V. and Thota, Niranjan and Sangwan, Payare L. and Malhotra, Pankaj and Ali, Furqan and Khan, Inshad A. and Chimni, Swapandeep S. and Koul, Surrinder (2010) Novel bisstyryl derivatives of bakuchiol: Targeting oral cavity pathogens. European Journal of Medicinal Chemistry, 45 (7). pp. 3125-3134. ISSN 02235234
 
Relation http://dx.doi.org/10.1016/j.ejmech.2010.03.049
http://iiim.csircentral.net/300/