Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591696 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
Benzobisthiazole derivatives were identified as novel helicase inhibitors through high throughput screening against purified Staphylococcus aureus (Sa) and Bacillus anthracis (Ba) replicative helicases. Chemical optimization has produced compound 59 with nanomolar potency against the DNA duplex strand unwinding activities of both B. anthracis and S. aureus helicases. Selectivity index (SIÂ =Â CC50/IC50) values for 59 were greater than 500. Kinetic studies demonstrated that the benzobisthiazole-based bacterial helicase inhibitors act competitively with the DNA substrate. Therefore, benzobisthiazole helicase inhibitors represent a promising new scaffold for evaluation as antibacterial agents.
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Authors
Bing Li, Ramdas Pai, Daniel Aiello, Ming Di, Marjorie H. Barnes, Norton P. Peet, Terry L. Bowlin, Donald T. Moir,