This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Infectious disease

Bacterial infection

Bacterial RNA polymerase

Computational and SAR studies suggest anthranilic acid compounds could be useful for treating Gram-positive bacterial infections. A structural model of bacterial RNA polymerase in complex with known inhibitors identified a theoretical pharmacophore predicted to have high inhibitory potency. Virtual screening and SAR studies identified anthranilic acid compounds with features corresponding to this pharmacophore. The best of these compounds showed in vitro potency against Gram-positive bacteria and lower rates of spontaneous resistance than the generic RNA polymerase inhibitor rifampicin. Next steps could include lead optimization and testing in animal models of bacterial infection.

SciBX 6(47); doi:10.1038/scibx.2013.1354
Published online Dec. 12, 2013

Patent and licensing status undisclosed

Hinsberger, S. et al. J. Med. Chem.; published online Oct. 11, 2013;
doi:10.1021/jm400485e
Contact: Rolf W. Hartmann, Saarland University, Saarbruecken, Germany
e-mail:
rolf.hartmann@helmholtz-hzi.de