Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus
IR@IIIM: CSIR-Indian Institute of Integrative Medicine, Jammu
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| Title |
Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus
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| Creator |
Thota, Niranjan
Reddy, Mallepally V. Kumar, Ashwani Khan, Inshad A. Sangwan, Payare L. Kalia, Nitin P. Koul, Jawahir L. Koul, Surrinder |
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| Subject |
Chemical Sciences
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| Description |
A new series of 3-(substituted-3,4-dihydronaphthyl)-2-propenoic acid amides has been prepared through convergent synthetic strategies and tested in combination with ciprofloxacin against NorA overexpressing Staphylococcus aureus 1199B as test strain for potentiating of the drug activity. Out of 24 compounds evaluated, 12 compounds potentiated the activity of ciprofloxacin and resulted in 2e16 fold reduction in the MIC (4e0.5 mg/mL) of the drug. The failure of these efflux pump inhibitors (EPIs) to
potentiate the activity of ciprofloxacin when tested against NorA knock out S. aureus SA-K1758 established
their identity as NorA inhibitors. The structure of all these newly synthesised compounds was confirmed by spectral data. The present communication describes the synthesis, bioevaluation, structure activity relationship and mechanism of action of these EPIs.
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| Date |
2010
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://iiim.csircentral.net/348/1/10.1016j.ejmech.2010.05.006.pdf
Thota, Niranjan and Reddy, Mallepally V. and Kumar, Ashwani and Khan, Inshad A. and Sangwan, Payare L. and Kalia, Nitin P. and Koul, Jawahir L. and Koul, Surrinder (2010) Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus. European Journal of Medicinal Chemistry, 45 (9). pp. 3607-3616. ISSN 02235234 |
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| Relation |
http://dx.doi.org/10.1016/j.ejmech.2010.05.006
http://iiim.csircentral.net/348/ |
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