The discovery of biaryl acids and amides exhibiting antibacterial activity against Gram-positive bacteria

Solid-phase synthetic methods for biaryl-based compounds were developed resulting in the construction of two 1000-member libraries. Numerous compounds were identified by high-throughput screening using whole cell screens to exhibit anti-microbial activity against Gram-positive bacteria. A series of...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 14; no. 6; pp. 1423 - 1426
Main Authors:	Look, Gary C., Vacin, Charles, Dias, Tracy M., Ho, Sun, Tran, Thuy H., Lee, Laurance L., Wiesner, Cedric, Fang, Flora, Marra, Andrea, Westmacott, Don, Hromockyj, Alexander E., Murphy, Martin M., Schullek, John R.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 22-03-2004 Elsevier
Subjects:	Amides - chemistry Amides - pharmacology Amino Acids - chemistry Amino Acids - pharmacology Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Escherichia coli - drug effects Escherichia coli - growth & development Gram-Positive Bacteria - drug effects Gram-Positive Bacteria - growth & development Medical sciences Microbial Sensitivity Tests - statistics & numerical data Pharmacology. Drug treatments Staphylococcus aureus - drug effects Staphylococcus aureus - growth & development α-Aminoacid Structure activity relation Gram positive bacteria Chlorine Organic compounds Chemical compound library Benzene derivatives Combinatorial chemistry Solid phase Antibacterial agent Chemical synthesis In vitro
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Summary:	Solid-phase synthetic methods for biaryl-based compounds were developed resulting in the construction of two 1000-member libraries. Numerous compounds were identified by high-throughput screening using whole cell screens to exhibit anti-microbial activity against Gram-positive bacteria. A series of biaryl compounds containing natural and unnatural amino acids were made to explore the SAR of the amino acid functionality. Biaryl-based compounds synthesized by solid-phase methods were shown to exhibit anti-microbial activity against Gram-positive bacteria in whole cell screens.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.01.026