Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6598-603. doi: 10.1016/j.bmcl.2013.10.058. Epub 2013 Nov 4.

Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors.

Author information

1
Biota Holdings Ltd, 10/585 Blackburn Road, Notting Hill, Victoria 3168, Australia. Electronic address: l.offermann@biota.com.au.

Abstract

The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties.

KEYWORDS:

Antibacterial; DNA gyrase; Topoisomerase

PMID:
24239017
DOI:
10.1016/j.bmcl.2013.10.058
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center