Summary information and primary citation
- PDB-id
-
5iwi;
DSSR-derived features in text and
JSON formats
- Class
- isomerase
- Method
- X-ray (1.98 Å)
- Summary
- 1.98a structure of gsk945237 with s.aureus DNA gyrase
and singly nicked DNA
- Reference
-
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown
P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM,
Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK,
Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN,
Pearson ND (2016): "Novel
tricyclics (e.g., GSK945237) as potent inhibitors of
bacterial type IIA topoisomerases."
Bioorg.Med.Chem.Lett., 26,
2464-2469. doi: 10.1016/j.bmcl.2016.03.106.
- Abstract
- During the course of our research on the lead
optimisation of the NBTI (Novel Bacterial Type II
Topoisomerase Inhibitors) class of antibacterials, we
discovered a series of tricyclic compounds that showed good
Gram-positive and Gram-negative potency. Herein we will
discuss the various subunits that were investigated in this
series and report advanced studies on compound 1
(GSK945237) which demonstrates good PK and in vivo efficacy
properties.
