86678-86-6Relevant articles and documents
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 (2018/07/25)
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.
Chemical modifications of bile acids under high-intensity ultrasound or microwave irradiation
Cravotto, Giancarlo,Boffa, Luisa,Turello, Marta,Parenti, Massimo,Barge, Alessandro
, p. 77 - 83 (2007/10/03)
High-intensity ultrasound (HIU) and microwave (MW) irradiation, having emerged as effective promoters of organic reactions, were exploited for the synthesis of bile acids derivatives. Esterification, amidation, hydrolysis, oxidation, and reduction were investigated. Compared to conventional methods, both techniques proved much more efficient, increasing product yields and dramatically cutting down reaction times. Scaled-up studies are now under way.
Antimicrobial activity of cholane compounds. Cholic and deoxycholic acids derivatives (Part 1)
Bellini,Quaglio,Guarneri,Cavazzini
, p. 185 - 190 (2007/10/02)
A series of compounds of (3 α, 5 β, 7 α, 12 α) 3, 7, 12-trihydroxy and (3 α, 5 β, 12 α) 3, 12-dihydroxy-cholanic acids was synthesized and their in vitro antibacterial activity was determined against a variety of Gram-negative and Gram-positive strains. Some of the compounds show an interesting antimicrobial activity against Gram-positive strains.
