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Citral derived amides as potent bacterial NorA efflux pump inhibitors

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  • Thota, Niranjan
  • Surrinder Koul
  • Mallepally V Reddy
  • Payare L Sangwan
  • Inshad A Khan
  • Ashwani Kumar
  • Alsaba F Raja
  • Samar S Andotra
  • Ghulam N Qazi

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.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind16
Udgave nummer13
Sider (fra-til)6535-43
Antal sider9
ISSN0968-0896
DOI
StatusUdgivet - 1 jul. 2008

ID: 189310052