Synthesis of functionalised 2-aryl-5-nitro-1H-indoles and their activity as bacterial NorA efflux pump inhibitors

S Samosorn, JB Bremner, A Ball, K Lewis

Index: Samosorn, Siritron; Bremner, John B.; Ball, Anthony; Lewis, Kim Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 3 p. 857 - 865

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Citation Number: 99

Abstract

In order to develop structure–activity relationships and to provide access to antibacterial agents for dual action studies, a variety of aryl group-substituted 2-aryl-5-nitro-1H-indoles were synthesized and the activity of the compounds assessed as inhibitors of the NorA multidrug resistance pump in the bacterium Staphylococcus aureus. The NorA protein from the major facilitator superfamily of efflux pumps confers resistance to a variety of ...