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Citral derived amides as potent bacterial NorA efflux pump inhibitors

IR@CSIR-IIIM

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Title Citral derived amides as potent bacterial NorA efflux pump inhibitors
 
Creator Thota, Niranjan
Koul, Surrinder
Reddy, Mallepally V.
Sangwan, Payare L.
Khan, Inshad A.
Kumar, Ashwani
Raja, Alsaba F.
Andotra, Samar S.
Qazi, Ghulam N.
 
Subject Chemical Sciences
Pharmacological Sciences
 
Description Monoterpene citral and citronellal have been used as starting material for the preparation of 5,9- dimethyl-deca-2,4,8-trienoic acid amides and 9-formyl-5-methyl-deca-2,4,8-trienoic acid amides. The amides on bioevaluation as efflux pump inhibitors (EPIs) against Staphylococcus aureus 1199 and NorA overexpressing S. aureus 1199B bacteria resulted in the identification of several of these as potent EPIs. Many of these amides have been shown to possess potency higher or equivalent to known EPIs such as reserpine, verapamil, carsonic acid, and piperine. In this communication, we report a convenient synthesis of alkenyl amides, their bioevaluation and identification as efflux pump inhibitors against S. aureus.
 
Date 2008
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://iiim.csircentral.net/231/1/10.1016j.bmc.2008.05.030.pdf
Thota, Niranjan and Koul, Surrinder and Reddy, Mallepally V. and Sangwan, Payare L. and Khan, Inshad A. and Kumar, Ashwani and Raja, Alsaba F. and Andotra, Samar S. and Qazi, Ghulam N. (2008) Citral derived amides as potent bacterial NorA efflux pump inhibitors. Bioorganic & Medicinal Chemistry, 16 (13). pp. 6535-6543. ISSN 09680896
 
Relation http://dx.doi.org/10.1016/j.bmc.2008.05.030
http://iiim.csircentral.net/231/