Bioorganic & Medicinal Chemistry 2008-07-01

Citral derived amides as potent bacterial NorA efflux pump inhibitors.

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

Index: Bioorg. Med. Chem. 16 , 6535-43, (2008)

Full Text: HTML

Abstract

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.

Related Compounds

  • Reserpine
  • Ciprofloxacin
  • Carnosic acid
  • Piperine

Related Articles:

Mechanisms involved in quinolone resistance in Mycoplasma mycoides subsp. capri.

2015-06-01

[Vet. J. 204 , 327-32, (2015)]

Multiple mutations and increased RNA expression in tetracycline-resistant Streptococcus pneumoniae as determined by genome-wide DNA and mRNA sequencing.

2015-07-01

[J. Antimicrob. Chemother. 70 , 1946-59, (2015)]

Deficiency of the novel exopolyphosphatase Rv1026/PPX2 leads to metabolic downshift and altered cell wall permeability in Mycobacterium tuberculosis.

2015-01-01

[MBio 6 , e02428, (2015)]

The phenolic diterpene totarol inhibits multidrug efflux pump activity in Staphylococcus aureus.

2007-12-01

[Antimicrob. Agents Chemother. 51 , 4480-3, (2007)]

LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.

2010-12-01

[Antimicrob. Agents Chemother. 54 , 5406-12, (2010)]

More Articles...