DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives

Roland W Bürli; Dustin McMinn; Jacob A Kaizerman; Wenhao Hu; Yigong Ge; Quinn Pack; Vernon Jiang; Matthew Gross; Martin Garcia; Richard Tanaka; Heinz E Moser

doi:10.1016/j.bmcl.2003.12.042

DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1253-7. doi: 10.1016/j.bmcl.2003.12.042.

Authors

Roland W Bürli¹, Dustin McMinn, Jacob A Kaizerman, Wenhao Hu, Yigong Ge, Quinn Pack, Vernon Jiang, Matthew Gross, Martin Garcia, Richard Tanaka, Heinz E Moser

Affiliation

¹ Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA.

PMID: 14980676
DOI: 10.1016/j.bmcl.2003.12.042

Abstract

Novel DNA minor-groove binding ligands with a promising antibacterial profile are described. Apart from excellent in vitro potency against multiple Gram-positive bacterial strains such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), and penicillin-intermediate Streptococcus pneumoniae (PISP), a small subset of compounds was active against Gram-negative bacteria such as Escherichia coli (E. coli).

Publication types

Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

Animals
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / metabolism*
Anti-Bacterial Agents / pharmacology
Benzimidazoles / chemistry
Benzimidazoles / metabolism*
Benzimidazoles / pharmacology
DNA / metabolism*
Drug Delivery Systems / methods*
Drug Resistance, Bacterial
Gram-Positive Bacteria / drug effects
Gram-Positive Bacteria / physiology
Ligands
Mice
Protein Binding

Substances

Anti-Bacterial Agents
Benzimidazoles
Ligands
DNA