Discovery of Diarylacrylonitriles as a Novel Series of Small Molecule Sortase A Inhibitors

On the basis of a hit from random screening, a novel class of small-molecule sortase A inhibitors was generated. The primary structure−activity relationship and the minimal structural requirements for potency were established through structural modifications and molecular modeling studies.

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Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2004-05, Vol.47 (10), p.2418-2421
Hauptverfasser:	Oh, Ki-Bong, Kim, Soo-Hwan, Lee, Jaekwang, Cho, Won-Jea, Lee, Taeho, Kim, Sanghee
Format:	Artikel
Sprache:	eng
Schlagworte:	Acrylonitrile - analogs & derivatives Acrylonitrile - chemical synthesis Acrylonitrile - chemistry Aminoacyltransferases - antagonists & inhibitors Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacterial Proteins Biological and medical sciences Cysteine Endopeptidases Kinetics Medical sciences Models, Molecular Pharmacology. Drug treatments Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	On the basis of a hit from random screening, a novel class of small-molecule sortase A inhibitors was generated. The primary structure−activity relationship and the minimal structural requirements for potency were established through structural modifications and molecular modeling studies.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm0498708