4XYC: Nanomolar Inhibitors Of Mycobacterium Tuberculosis Glutamine Synthetase 1: Synthesis, Biological Evaluation And X-ray Crystallographic Studies

A series of imidazo[1,2-a]indeno[1,2-e]pyrazin-4-ones that potently inhibit M. tuberculosis glutamine synthetase (GlnA1) has been identified by high throughput screening. Exploration of this series was performed owing to a short chemistry program. Despite possibly nanomolar inhibitions, none of these compounds was active on whole cell Mtb, suggesting that GlnA1 may not be a suitable target to find new anti-tubercular drugs.
PDB ID: 4XYCDownload
MMDB ID: 128143
PDB Deposition Date: 2015/2/2
Updated in MMDB: 2015/04
Experimental Method:
x-ray diffraction
Resolution: 3.3  Å
Source Organism:
Similar Structures:
Biological Unit for 4XYC: dodecameric; determined by author and by software (PISA)
Molecular Components in 4XYC
Label Count Molecule
Proteins (12 molecules)
Glutamine Synthetase 1
Molecule annotation
Chemicals (12 molecules)
* Click molecule labels to explore molecular sequence information.

Citing MMDB