6912-96-5Relevant academic research and scientific papers
The Design, Synthesis, and Characterizations of Spore Germination Inhibitors Effective against an Epidemic Strain of Clostridium difficile
Sharma, Shiv K.,Yip, Christopher,Esposito, Emilio Xavier,Sharma, Prateek V.,Simon, Matthew P.,Abel-Santos, Ernesto,Firestine, Steven M.
, p. 6759 - 6778 (2018)
Clostridium difficile infections (CDI), particularly those caused by the BI/NAP1/027 epidemic strains, are challenging to treat. One method to address this disease is to prevent the development of CDI by inhibiting the germination of C. difficile spores. Previous studies have identified cholic amide m-sulfonic acid, CamSA, as an inhibitor of spore germination. However, CamSA is inactive against the hypervirulent strain R20291. To circumvent this problem, a series of cholic acid amides were synthesized and tested against R20291. The best compound in the series was the simple phenyl amide analogue which possessed an IC50 value of 1.8 μM, more than 225 times as potent as the natural germination inhibitor, chenodeoxycholate. This is the most potent inhibitor of C. difficile spore germination described to date. QSAR and molecular modeling analysis demonstrated that increases in hydrophobicity and decreases in partial charge or polar surface area were correlated with increases in potency.
A NEW DERIVATIZATION FOR THE SPECTROPHOTOMETRIC DETERMINATION OF CARBOXYL GROUPS
Goeroeg, S.,Renyei, M.
, p. 65 - 70 (2007/10/02)
A new derivatization is described for the spectrophotometric determination of carboxyl groups.The reagent is diethyl anilinophosphite which is prepared in situ from diethyl chlorophosphite and aniline.With the aid of this reagent carboxylic acids are quantitatively transformed to the carboxanilides which possess favourable spectrophotometric properties (λmax about 242 nm; ε = 14000).A great variety of fatty acids and bile acids has been determined by this method.The reaction leading to the chromophoric derivative is completed within 60 minutes at 100 deg C using butyronitrile as solvent.The spectrophotometric measurement is carried out in 0.1 N ethanolic hydrochloric acid, where the excess reagent is decomposed and the small absorbance of the protonated aniline results in a low reagent blank.The relative standard deviations obtained by this method range between 0.82 and 1.59 percent.The possiblity of extending the application of the reagent and the potential use of other aniline and aromatic amine derivatives in chromatography are also discussed.
