Article
New inhibitors of bacterial protein synthesis from a combinatorial library of macrocycles.
Journal of medicinal chemistry - 1 Aug 2002
Jefferson Elizabeth A, Arakawa Satoshi, Blyn Lawrence B, Miyaji Alycia, Osgood Stephen A, Ranken Raymond, Risen Lisa M, Swayze Eric E
Abstract excerpt
A mixture-based combinatorial library of 14-membered macrocycles was synthesized to target ribosomal RNA and uncover a new class of antibacterial agents. High-throughput screening identified a macrocyclic mixture that inhibited cell-free-coupled transcription/translation in Escherichia coli-derived extracts, with an IC(50) value in the 25-50 microM range. In a follow-up library of 64 single macrocycles, 8 gave...
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