طريقة جديدة لتحضير حامض الكينو دي اوكسي كوليك بالمواصفات الدوائية الدستورية و دراسة تاثيره كمضاد بكتيري

A new method for the synthesis of chenodeoxycholic acid (3,7- Dihydroxy-5ß-cholanic acid) with pharmaceutical specification, was established. It include the conversion of Methyl 3,7-Diacetoxy-12 - ketocholate to Methyl 3,7-diacetoxy-12-oxocholate tosylhydrazone. This compound was reduced with potassium tetrahydroborate to the counter methyl ester, which undergoes hydrolysis to chenodeoxycholic acid, finally purified by recrysallization with acetonitrile (with a yield of 60 %). This method offer the following advantages: reducing the number of synthesis steps and the formation of unwanted isomers, as well as its suitability for large scale production. The bactericidal effect of Chenodeoxycholic acid and its intermediate derivatives were studied by using locally isolated strains of the following bacteria: P. aeruginosa ، E. coli ،S. aureus، and S. epidermidis by following Broth dilution method. The results showed that these compounds posses bactericidal effect very clear for Gram- positive bacteria particularly in case of S. epidermidis. It was found that Methyl 3,7- diacetoxy-12-oxocholate tosylhydrazone (IV) showed relatively the highest bactericidal effect, probably due to the presence of sulphonyl effect.