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Bioorg Med Chem Lett. 2007 May 15;17(10):2807-10. Epub 2007 Feb 25.

Small molecule inhibitors of E. coli primase, a novel bacterial target.

Author information

1
Achillion Pharmaceuticals, 300 George Street, New Haven, CT 06511, USA.

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.

PMID:
17350255
DOI:
10.1016/j.bmcl.2007.02.056
[Indexed for MEDLINE]

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