3217-44-5Relevant academic research and scientific papers
Identification and Structure-Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli
Haynes, Keith M.,Abdali, Narges,Jhawar, Varsha,Zgurskaya, Helen I.,Parks, Jerry M.,Green, Adam T.,Baudry, Jerome,Rybenkov, Valentin V.,Smith, Jeremy C.,Walker, John K.
, p. 6205 - 6219 (2017/08/02)
In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics. Small molecule 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 experimental screening and in silico virtual screening, we recently identified novel classes of EPIs that interact with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli. Herein, we present initial optimization efforts and structure-activity relationships around one of those previously described hits, NSC 60339 (1). From these efforts we identified two compounds, SLUPP-225 (17h) and SLUPP-417 (17o), 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 1, and potentiation of the activity of novobiocin and erythromycin.
DIMERIC COMPOUNDS
-
Page/Page column 51, (2014/07/07)
Disclosed are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein Z, X, Q and R1 are as described in this application, and methods of using the compounds in the treatment of cancer.
Polyesters of poly(oxyalkylene) hydroxyaromatic ethers
-
, (2008/06/13)
Poly(oxyalkylene) hydroxyaromatic ethers having the formula: STR1 or a fuel-soluble salt thereof; where n is an integer from 5 to 100; x is an integer from 0 to 10; R1 and R2 are each independently hydrogen, hydroxy, lower alkyl havi
