Novel Anti-bacterials Against MRSA: Synthesis of Focussed Combinatorial Libraries of Tri-Substituted 2(5H)-Furanones

Author(s): Eric Lattmann, Nison Sattayasai, Carl S. Schwalbe, Suwanna Niamsanit, David C. Billington, Pornthip Lattmann, Christopher A. Langley, Harjit Singh, Simon Dunn

Journal Name: Current Drug Discovery Technologies

Volume 3 , Issue 2 , 2006

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Mucobromic and mucochloric acid were used as building blocks for the construction of a chemical combinatorial library of 3,4,5-trisubstituted 2(5H)-furanones. With these 2 butenolide building blocks, and eight alcohols a sublibrary of 16 dihalogenated 5-alkoxy-2(5H)-furanones was prepared. This sublibrary of 5-alkoxylated furanones was reacted with 16 amines generating a full size focussed combinatorial library of 256 individual compounds. This three dimensional combinatorial library of 3-halogen-4-amino-5-alkoxy-2(5H)-furanones was prepared around the benzimidazolyl furanone lead structure by applying a solution phase combinatorial chemistry concept. Typical representatives of the library were purified and fully characterized and one x-ray structures was recorded, additionally. The 3-bromo-4-benzimizazolyl-5-methoxy-2(5H)furanone, Br-A-l, showed an MIC of 8 g/ml against the multiresistant Staphylococcus aureus ( MRSA).

Keywords: Focussed combinatorial library, butenolides, 4-amino-5-alkoxy-2(5H)-furanones, antibacterials structure, MRSA

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Article Details

Year: 2006
Page: [125 - 134]
Pages: 10
DOI: 10.2174/157016306778108857
Price: $65

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