- SYNTHESIS OF GLYCOCONJUGATE DERIVATIVES OF A BILE ACID
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Processes for the synthesis and purification of glycoconjugate derivatives of cholic acid are provided herein.
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Paragraph 0086-0087; 0091
(2021/04/10)
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- Cholic acid derivative with antibacterial activity and pharmaceutical composition thereof
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The invention provides a compound shown as formula (I), or a stereoisomer, or a salt, or a solvate, or a prodrug, or a metabolite thereof. The compound can effectively inhibit the growth of clostridium difficile thalli, has remarkable antibacterial activity, and has a very promising application prospect in preparing medicines for preventing and/or treating clostridium difficile infectious diseases, recurrence of clostridium difficile infectious diseases or complications of clostridium difficile infectious diseases.
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Paragraph 0209-0211; 0213
(2020/03/25)
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- Synthesis, anticancer activities, antimicrobial activities and bioavailability of berberine-bile acid analogues
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Fifteen berberine-bile acid analogues were synthesized. Anticancer activities of these analogues compared with berberine (BBR) were evaluated in vitro; among the analogues, A4, B4, and B5 had higher cytotoxicity than that of BBR. Most of the analogues showed higher antimicrobial activity against Staphylococcus aureus ATCC 25923 and Staphylococcus albus ATCC 8799 than that of BBR, but Bacillus subtilis AS 1.398 and Escherichia coli ATCC 31343 were not sensitive to all of the analogues. A4 and B4 were stable in the serum stability assay. B4 showed promising oral bioavailability in mice.
- Li, Qingyong,He, Wuna,Zhang, Li,Zu, Yuangang,Zhu, Qiaochu,Deng, Xiaoqiu,Zhao, Tengfei,Gao, Wenqing,Zhang, Baoyou
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scheme or table
p. 573 - 580
(2012/08/08)
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- METHOD FOR THE SYNTHESIS OF GLYCOCHOLIC ACID
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Process for preparing glycocholic acid comprising the following steps: a) making a mixed anhydride of cholic acid through the suspension of cholic acid in acetone or in aqueous acetone in presence of a base, and subsequent reaction with an alkyl chloroformate; b) aminolysis of the so obtained mixed anhydride of cholic acid with an aqueous solution of a glycine ester, resulting in an ester of glycocholic acid; c) hydrolysis of the ester of glycocholic acid thus obtained through the treatment with aqueous soda or aqueous potassium and precipitation of glycocholic acid through acidification of the corresponding sodium salt.
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Page/Page column 6
(2010/11/18)
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- An improved procedure for the synthesis of glycine and taurine conjugates of bile acids
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Glycine and taurine conjugates of 5β cholanic acids have been synthesized using improved procedures based on the peptide coupling reagent, N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline. The conjugates are obtained in chromatographically pure form in yields higher than 90%. The use of this procedure in the large scale preparation of choly[1,2 13C2]glycine is described.
- Tserng,Hachey,Klein
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p. 404 - 407
(2007/10/06)
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