胡椒碱 反应 2.5H,反应生成 胡椒碱 参考文献:Vicinal Difluorination As A C=c Surrogate: An Analog Of Piperine With Enhanced Solubility,Photostability,And Acetylcholinesterase Inhibitory Activity 标题:Vicinal Difluorination As A C=c Surrogate: An Analog Of Piperine With Enhanced Solubility,Photostability,And Acetylcholinesterase Inhibitory Activity 摘要:胡椒碱是一种从花椒中提取的天然产物,具有多种生物活性,是一种极具吸引力的药物化学先导化合物.然而,胡椒碱的理化性质存在一些问题,包括水溶性差和容易受紫外线诱导降解.在这项研究中,我们设计了一种哌啶类似物,其中的中心共轭烃链被一个二氟烷基取代.我们的研究表明,这种含氟哌啶类似物具有更优越的理化性质,而且对一个特定的药物靶点--乙酰胆碱酯酶--具有更高的效力和选择性.这项工作凸显了三代二氟烷基作为 E-烯的替代物在药物化学中的潜在用途. DOI:10.3762/bjoc.16.216
专利号:WO-2024181781-A1 优先权日:2023-02-27 标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same 发明人:JANG MYOUNG HOON; CHOI JAE SUN 权利人:SP2 TX INC 摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.
专利号:US-5962515-A 优先权日:1997-05-29 标题 :Process for isolation and synthesis of 1-(3,4 methylenedioxy-phenyl)-1E-tetradecene and its analogues and their activities against tumors and infections 发明人:UPADHYAY SHAKTI N; VISHWAKARMA RAM A; GHOSAL SABARI; SHUKLA SUPRIYA; BOSE CHANDA; KAMRA ANITA 权利人:NAT INST IMMUNOLOGY 摘要:Process for isolation of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene from Piper longum. Processes for synthesis of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene; its stereoisomers and analogues are disclosed. The compounds isolated and synthesized according to this invention have immunomodulatory properties and can be used to treat tumors and infections.
专利号:US-2021315830-A1 优先权日:2018-08-31 标题 :A curcumin loaded stabilized polymeric nanoparticles with increased solubility and photo-stability and a green process for the synthesis thereof 发明人:ACHARYA AMITABHA; KUMARI AVNESH; GULIANI ANIKA; KUMAR SANJAY 权利人:COUNCIL SCIENT IND RES 摘要:The present invention explored PLGA NPs synthesis using plant extracts as surfactants by nanoprecipitation process. PLGA NPs synthesized using Camellia sinensis, Dendrocalamus hamiltonii, Ficus palmata and Rubus ellipticus leaf extracts were further explored for encapsulation, controlled and sustained release of well-known antioxidant molecule, curcumin. This plant extract based nanoprecipitation process for the synthesis of PLGA NPs can be further explored for encapsulation of many other antioxidant molecules of therapeutic importance.
专利号:US-11634741-B2 优先权日:2013-11-20 标 题:Synthesis of L-nucleic acids by means of an enzyme 发明人:PECH ANDREAS; JAROSCH FLORIAN; JAHNZ MICHAEL; KLUSSMANN SVEN; DAVID RALF 权利人:APTARION BIOTECH AG 摘要:The present invention is related to a method for adding one or more L-nucleotides to the 3′end of a first L-nucleic acid, wherein the method comprises the step of reacting the one or more L-nucleotides with the first L-nucleic acid in the presence of a protein comprising a mutant enzymatic activity exhibiting moiety, wherein the enzymatic activity is capable of adding one or more L-nucleotides to the 3′ end of the first L-nucleic acid, wherein the mutant enzymatic activity exhibiting moiety comprises an amino acid sequence, wherein the amino acids of the amino acid sequence are D-amino acids, wherein the mutant enzymatic activity exhibiting moiety is a variant of an enzymatic activity exhibiting moiety, wherein the enzymatic activity exhibiting moiety consists of an amino acid sequence according to SEQ ID NO: 15 and wherein the amino acids of the amino acid sequence according to SEQ ID NO: 15 are D-amino acids, wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety differs from the amino acid sequence of the enzymatic activity exhibiting moiety consisting of an amino acid sequence according to SEQ ID NO: 15 at least at one amino acid position, preferably at three amino acid positions, and/or wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety is a truncated form of an amino acid sequence according to SEQ ID NO: 15, and wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety is different from an amino acid sequence according to any of SEQ ID NOs 15 to 22 and 51.
专利号:US-9850471-B2 优先权日:2012-05-16 标题:Enzymatic synthesis of L-nucleic acids 发明人:PECH ANDREAS; DAVID RALF; JAROSCH FLORIAN; JAHNZ MICHAEL; KLUSSMANN SVEN 权利人:NOXXON PHARMA AG 摘要:The invention relates to a method of reacting one or more L-nucleotides with a first L-nucleic acid in the presence of a D-enzyme that adds the one or more L-nucleotides to the 3′ end of the first L-nucleic acid.
专利号:US-2019276389-A1 优先权日:2015-12-18 标题:Synthesis of aryl cyclohexane ester derivatives useful as sensates in consumer products 发明人:WOS JOHN AUGUST; YELM KENNETH EDWARD; BUNKE GREGORY MARK; FREDERICK HEATH ALAN; REILLY MICHAEL; HAUGHT JOHN CHRISTIAN; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
参考文献:10.1016/s0968-0896(02)00130-x 摘要:Tsukamoto S, Tomise K, Miyakawa K, Cha B, Abe T, Hamada T, Hirota H, Ohta T. CYP3A4 Inhibitory Activity of New Bisalkaloids, Dipiperamides D and E, and Cognates from White Pepper. Bioorganic & Medicinal Chemistry. 2002 Sep;10(9):2981–5. doi: 10.1016/s0968-0896(02)00130-x.