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طريقةجديدة لتحضير حامض الكينودي اوكسي كوليك بالمواصفات الدوائية الدستورية ودراسة تأثيره كمضاد بكتيري

Authors: سعدي محمد ظاهر --- سوزان سعدي حسين
Journal: Journal of College of Education مجلة كلية التربية ISSN: 18120380 Year: 2009 Issue: 3 Pages: 419-441
Publisher: Al-Mustansyriah University الجامعة المستنصرية

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Abstract

Anervmethodfortlresynthesisofchenodeoxycholicacid(3,7-Dilrydroxy-5B-cholanicacitl)withpharmaceuticalspecification,wasesttrblished.ItincludetheconversionofMethyls,T.Diacetoxy.l2.ketocholate to Methyl 3,7-diacetoxy-12-oxocholate tosylhydrazone'Tlriscompoundwasreducedwithpotassiumtetrahydroboratetotlrecountermethylester,whichundergoeshydrotysistochenodeoxycholicacid,finaltypurifiedbyrecrysallizationwithacetonitrile(withayieldof 60 %). This methoi offer the following advantages: reducing thenumberofsynthesisstepsandtheformationofunwantedisomers,asvvell as its suitability for large scale production'The bactericiial effect of chenodeoxycholic acid and itsintermediatederivativeswerestudiedbyusinglocallyisolatedstrains ofthe following bacteria P' aeruginosa ' E' coli 'S' aureusr aud s'epidermidis by following Broth dilution method. The results showedthat these compounds posses bactericidal cffect very clear for Gratnpositivebacteria parlicularly in case of S. epidermidis. It was foundthat Methyl 3,7 - diacetoxy- I 2-oxocholate tosylh y drazone (IV) showedrelatively the highest bactericidal effect, probably due to the presence ofsulphonyl effect.

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