胆酸置于盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,聚甘氨酸体系中,用 二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应 8.0H,反应生成 甘氨胆酸 参考文献:Synthesis,Anticancer Activities,Antimicrobial Activities And Bioavailability Of Berberine-Bile Acid Analogues 标题:Synthesis,Anticancer Activities,Antimicrobial Activities And Bioavailability Of Berberine-Bile Acid Analogues 摘要:合成了十五种小檗碱-胆酸类似物.与小檗碱(bbr)相比,这些类似物的抗癌活性在体外进行了评估;在这些类似物中,A4,B4 和 B5 的细胞毒性高于 Bbr.大多数类似物对金黄色葡萄球菌 Atcc 25923 和白色念珠菌 Atcc 8799 具有较高的抗菌活性,而对枯草芽孢杆菌 As 1.398 和大肠杆菌 Atcc 31343 则无敏感性.a4 和 B4 在血清稳定性实验中表现出稳定性.b4 在小鼠中显示出非常好的口服生物利用度. DOI:10.2174/157018012800673010
专利信息
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-2012190064-A1 优先权日:2004-10-01 标题 :Feeding buffers, systems, and methods for in vitro synthesis of biomolecules 发明人:KUDLICKI WIESLAW ANTONI; KEPPETIPOLA SHIRANTHI; FLETCHER JULIA; GETBEHEAD ASHLEY ELAINE; KATZEN FEDERICO; VOZZA-BROWN LAURA 权利人:KUDLICKI WIESLAW ANTONI; KEPPETIPOLA SHIRANTHI; FLETCHER JULIA; GETBEHEAD ASHLEY ELAINE; KATZEN FEDERICO; VOZZA-BROWN LAURA; LIFE TECHNOLOGIES CORP 摘要:Compositions, methods and kits for in vitro systems for synthesis of biomolecules such as polypeptides, are provided herein. Cell extracts that provide enhanced yields of soluble proteins using in vitro protein synthesis methods are provided. The invention also includes methods for producing high yields of proteins by the addition of a feeding solution that includes amino acids and an energy source to an ongoing in vitro synthesis system. The invention also includes methods of using a high-yield in vitro synthesis system to produce large quantities of proteins with incorporated labeled amino acids for analysis by methods such as by NMR. The invention further includes vectors for enhanced production of proteins from nucleic acid templates using in vitro synthesis systems.
专利号:US-7202256-B2 优先权日:2004-04-14 标题:Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 发明人:GU JIANXIN; RUPPEN MARK E; RAVEENDRANATH PANOLIL; CHEW WARREN; SHAW CHIA-CHENG 权利人:WYETH CORP 摘要:Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
专利号:US-2006211083-A1 优先权日:2005-01-21 标题:Products and processes for in vitro synthesis of biomolecules 发明人:KATZEN FEDERICO; KUDLICKI WIESLAW; FLETCHER JULIA 权利人:KATZEN FEDERICO; KUDLICKI WIESLAW; FLETCHER JULIA 摘要:Provided herein are products and processes for efficiently synthesizing biomolecules in vitro using cell-free extracts derived from mammalian cells and insect cells. In an embodiment, provided is a process for preparing a cell-free extract from insect cells and mammalian cells that efficiently synthesizes post-translationally modified target proteins (e.g., glycosylated target proteins). In some embodiments, a ribonucleic acid is synthesized in vitro that comprises a cap, a 5′ untranslated region comprising an 18S rRNA binding ribonucleotide sequence, and a target ribonucleotide sequence. It has been determined that such ribonucleic acids result in efficient in vitro synthesis of a target protein using cell-free extracts derived from non-rabbit mammalian cells and insect cells.
专利号:US-9828445-B1 优先权日:2016-12-13 标题:Synthesis of modified chitosan particles for oral insulin delivery 发明人:ATTA AYMAN M; AL-LOHEDAN HAMAD A; EZZAT ABDELRAHMAN O 权利人:UNIV KING SAUD 摘要:Synthesis of modified chitosan particles for oral insulin delivery includes amidation of chitosan with a fatty acid, a modified fatty acid, and/or an amino acid. The amidated chitosan can be grafted with N-isopropylacrylamide (NIPAm) and cross-linked to provide the modified chitosan particles.
专利号:US-9683007-B2 优先权日:2009-12-18 标 题 :Methods for the purification of deoxycholic acid 发明人:MORIARTY ROBERT M; PRASAD ACHAMPETA RATHAN; REID JOHN GREGORY; SWARINGEN JR ROY A 权利人:KYTHERA BIOPHARMACEUTICALS INC 摘要:Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-α-hydroxysteroids from Δ-9,11-ene, 11-keto or 11-hydroxy-β-steroids. This inversion is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
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合成参考文献
参考文献:10.1371/journal.pone.0022094 摘要:Trottier J, Białek A, Caron P, Straka RJ, Milkiewicz P, Barbier O. Profiling Circulating and Urinary Bile Acids in Patients with Biliary Obstruction before and after Biliary Stenting. PLoS ONE. 2011 Jul 08;6(7):e22094. doi: 10.1371/journal.pone.0022094.