Haynes, Keith M. published the artcileIdentification and Structure-Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli, Category: imidazoles-derivatives, the publication is Journal of Medicinal Chemistry (2017), 60(14), 6205-6219, database is CAplus and MEDLINE.
In Gram-neg. bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics. Small mol. adjuvants that act as efflux pump inhibitors (EPIs) have the potential to reinvigorate existing antibiotics that are currently ineffective due to efflux mechanisms. Through a combination of rigorous exptl. screening and in silico virtual screening the authors recently identified novel classes of EPIs that interact with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in E. coli. Herein, the authors present initial optimization efforts and structure-activity relationships around one of those previously described hits, NSC 60339. From these efforts the authors identified two compounds, SLUPP-225 (II) and SLUPP-417 (III), which demonstrate favorable properties as potential EPIs in E. coli cells including the ability to penetrate the outer membrane, improved inhibition of efflux relative to (I) and potentiation of the activity of novobiocin and erythromycin.
Journal of Medicinal Chemistry published new progress about 13682-33-2. 13682-33-2 belongs to imidazoles-derivatives, auxiliary class Imidazole,Amine,Benzene, name is 4-(1H-Imidazol-2-yl)aniline, and the molecular formula is C9H9N3, Category: imidazoles-derivatives.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem