Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366703 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
Bacterial primase is essential for DNA replication in Gram-positive and Gram-negative bacteria. It is also structurally distinct from eukaryotic primases, and therefore an attractive, but under-explored, target for therapeutic intervention. We applied virtual screening to discover primase inhibitors, and subsequently several commercially available analogs of these initial hits showed potent primase inhibition and in vitro antibacterial activity. This work provides a 3D pharmacophore for primase ligands, SAR trends, and leads that can be further optimized.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Atul Agarwal, Shirley Louise-May, Jane A. Thanassi, Steven D. Podos, Jijun Cheng, Christy Thoma, Cuixian Liu, Jason A. Wiles, David M. Nelson, Avinash S. Phadke, Barton J. Bradbury, Milind S. Deshpande, Michael J. Pucci,