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Discovery of Novel Antibacterial Agents Active Against Methicillin‐Resistant Staphylococcus aureus from Combinatorial Benzopyran Libraries
Author(s) -
Nicolaou K. C.,
Roecker A. J.,
Barluenga Sofia,
Pfefferkorn Jeffrey A.,
Cao GuoQiang
Publication year - 2001
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/1439-7633(20010601)2:6<460::aid-cbic460>3.0.co;2-2
Subject(s) - staphylococcus aureus , benzopyran , combinatorial synthesis , combinatorial chemistry , antibacterial activity , chemistry , in vitro , antibacterial agent , chemical library , stereochemistry , microbiology and biotechnology , biology , bacteria , antibiotics , biochemistry , small molecule , genetics
In vitro antibacterial potencies similar to that of vancomycin against several strains of methicillin‐susceptible and ‐resistant Staphylococcus aureus were found for some novel benzopyran‐derived antibacterial agents (see picture; R=H, t Bu; X=O, S). Lead compounds were identified from compound libraries, generated by split‐and‐pool combinatorial synthesis, by using high‐throughput antibacterial screening. A preliminary optimization was achieved by molecular fine‐tuning through design and chemical synthesis followed by further biological testing.