专利号:WO-2020032913-A1 优先权日:2018-08-04 标题:Process for synthesis of oroxylin a 发明人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; RAMANUJAM RAJENDRAN; HEMANTHA HOSAHALLI 权利人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; RAMANUJAM RAJENDRAN; HEMANTHA HOSAHALLI PRABHAKARA 摘要:Disclosed is a novel, simple, scalable and environment friendly process for the synthesis of Oroxylin A from Baicalin. Baicalm is esterified to obtain a methyl ester which is further selectively methylated to provide Oroxylin A gluciironide methyl ester which on de- glycosylation results in the formation of Oroxylin A.
专利号:US-2009221568-A1 优先权日:2005-11-04 标题:Synthesis of Inhibitors of FtsZ 发明人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY 权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY 摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.
专利号:WO-2025081225-A1 优先权日:2023-10-17 标 题 :Synthesis of polyphenols 发明人:TURLAND CADE LACHLAN; GROLMAN DAVID; BEHRENDORFF JAMES BRUCE YARNTON HAYCOCK; MORADI SHAYLI VARASTEH; THOMSON RAINE ELIZABETH STURT 权利人:Delica Therapeutics Pty Ltd 摘要:The present disclosure relates to polyphenols, including flavonoids, flavones and cannflavins, and methods of synthesising polyphenols. The present disclosure provides methods, enzymes and compositions that may be useful in the synthesis of polyphenols.
专利号:US-10407401-B1 优先权日:2018-08-04 标题 :Process for synthesis of Oroxylin A 发明人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; RAMANUJAM RAJENDRAN; HEMANTHA HOSAHALLI PRABHAKARA 权利人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; RAMANUJAM RAJENDRAN; HEMANTHA HOSAHALLI PRABHAKARA; SAMI LABS LTD 摘要:Disclosed is a novel, simple, scalable and environment friendly process for the synthesis of Oroxylin A from Baicalin. Baicalin is esterified to obtain a methyl ester which is further selectively methylated to provide Oroxylin A glucuronide methyl ester which on de-glycosylation results in the formation of Oroxylin A.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-2024026314-A1 优先权日:2020-11-25 标题 :Polypeptides for use in the synthesis of bioactive phenolic compounds 发明人:ROTHSTEIN STEVEN; AKHTAR TARIQ; CASARETTO JOSE; PERRIN COLBY; VAN GELDER KRISTEN 权利人:ROTHSTEIN STEVEN; AKHTAR TARIQ; CASARETTO JOSE; PERRIN COLBY; VAN GELDER KRISTEN 摘要:Described herein is a polypeptide encoding a prenyltransferase for prenylating a polyphenol and a polypeptide encoding an O-methyltransferase for methylating a polyphenol. For example, the polypeptide comprises or consists of the sequence of SEQ ID NO: 1, 2, 3, 4, 5, and/or 6, and/or a polypeptide listed in Table 1, and/or SEQ ID NO: 7-30, or a variant thereof having at least 80% sequence identity to SEQ ID NO: 1, 2, 3, 4, 5, and/or 6, and/or the polypeptide listed in Table 1, and/or SEQ ID NO: 7-30, or a fragment of the polypeptide or the variant thereof.
1: Jiang Y, Gong FL, Zhao GB, Li J. Chrysin suppressed inflammatory responses and the inducible nitric oxide synthase pathway after spinal cord injury in rats. Int J Mol Sci. 2014 Jul 10;15(7):12270-9. doi: 10.3390/ijms150712270. doi: 10.3390/ijms150711510. doi: 10.1016/j.taap.2014.05.018. [Epub ahead of print] doi: 10.1016/j.taap.2014.05.007. Epub 2014 May 18. doi: 10.1007/s11418-014-0840-1. Epub 2014 May 1. doi: 10.1016/j.bcp.2014.03.016. Epub 2014 Apr 2. doi: 10.1016/j.ejpb.2014.03.011. Epub 2014 Mar 29.
合成参考文献
参考文献:10.1186/1475-2891-10-73 摘要:Bojić M, Debeljak Ž, Tomičić M, Medić-Šarić M, Tomić S. Evaluation of antiaggregatory activity of flavonoid aglycone series. Nutrition Journal. 2011 Jul 11;10(1):73. doi: 10.1186/1475-2891-10-73. 参考文献:10.1016/j.freeradbiomed.2011.06.021 摘要:Bensasson RV, Zoete V, Jossang A, Bodo B, Arimondo PB, Land EJ. Potency of inhibition of human DNA topoisomerase I by flavones assessed through physicochemical parameters. Free Radic Biol Med. 2011 Oct 01;51(7):1406–10. doi: 10.1016/j.freeradbiomed.2011.06.021. 参考文献:10.1021/np50001a002 摘要:Edwards JM, Raffauf RF, Le Quesne PW. Antineoplastic activity and cytotoxicity of flavones, isoflavones, and flavanones. J Nat Prod. 1979 Jan;42(1):85–91. doi: 10.1021/np50001a002. 参考文献:10.4103/0971-4065.82131 摘要:Boutabet K, Kebsa W, Alyane M, Lahouel M. Polyphenolic fraction of Algerian propolis protects rat kidney against acute oxidative stress induced by doxorubicin. Indian J Nephrol. 2011 Apr;21(2):101–6. 参考文献:10.1038/cddis.2011.66 摘要:Polier G, Ding J, Konkimalla BV, Eick D, Ribeiro N, Köhler R, Giaisi M, Efferth T, Desaubry L, Krammer PH, Li-Weber M. Wogonin and related natural flavones are inhibitors of CDK9 that induce apoptosis in cancer cells by transcriptional suppression of Mcl-1. Cell Death & Disease. 2011 Jul 21;2(7):e182. doi: 10.1038/cddis.2011.66.