📜对羟基苯乙腈置于盐酸,三氟化硼乙醚,甲基磺酰氯体系中,用 乙醚 作为反应溶剂,化学反应 27.0H,反应生成 鸢尾黄素 参考文献:Polyphenols Based On Isoflavones As Inhibitors Of Helicobacter Pylori Urease 标题:Polyphenols Based On Isoflavones As Inhibitors Of Helicobacter Pylori Urease 摘要:Twenty Polyphenols Were Synthesized And Evaluated For Their Effect On Helicobacter Pylori Urease. Among These Compounds,4-(P-Hydroxyphenethyl)Pyrogallol (15) (Ic50 = 0.03 Mm) And 7,8,4'-Trihydroxyisoflavone (19) (Ic50 = 0.14 Mm) Showed Potent Inhibitory Activities,And Inhibited Helicobacter Pylori Urease In A Time-Dependent Manner. The Structure-Activity Relationship Of These Polyphenols Revealed: The Two Ortho Hydroxyl Groups Were Essential For Inhibitory Activity Of Polyphenol. When The C-Ring Of Isoflavone Was Broken,The Inhibitory Activity Markedly Decreased. As For Deoxybenzoin,The Carboxyl Group Was Clearly Detrimental. (C) 2007 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmc.2007.03.045
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-2022133840-A1 优先权日:2020-10-30 标题:Use of microcystin in preparation of drug for preventing or treating organ and tissue fibrosis diseases 发明人:WANG YAPING; XU LIZHI; WANG JIE; Zhao qingya 权利人:NANJING UNIVERSITY OF TECHNOLOGY 摘要:Use of microcystins having a monocyclic heptapeptide structure in preparation of drugs for preventing or treating organ and tissue fibrosis diseases. Preferably, the microcystins are microcystin-LR with amino acids at positions 2 and 4 of a monocyclic heptapeptide structure thereof being leucine and arginine respectively, or are microcystin-RR with amino acids at positions 2 and 4 thereof being both arginine. Also provided is a method for inhibiting myofibroblast differentiation and collagen synthesis. The method is implemented by inhibiting a TGF-β/Smad signaling pathway by using one or more microcystins.
专利号:US-2007232495-A1 优先权日:2006-03-24 标题:Compositions and methods to add value to plant products, increasing the commercial quality, resistance to external factors and polyphenol content thereof 发明人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 权利人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 摘要:The invention is related to compositions and methods that naturally protect plant tissues against ultraviolet radiation and temperature, thus giving protection against sunburn to plants, plant parts, fruits and/or flowers during their development. The invention is also related to compositions and methods to naturally improve the color of plants, plant parts, fruits and/or flowers by inducing the natural synthesis of flavonoids and anthocyanins present in plants. Likewise, the present invention is directed to improving the nutritional value of plants, plant parts, fruits and/or flowers by increasing the normal levels of polyphenolic compounds, especially flavonoids, present therein. Additionally, the present invention is related to compositions and methods that give more resistance to plants, plant parts, fruits and/or flowers against pathogens as bacteria and fungi. Finally, the present invention is related to plants, plant parts, fruits, flowers and/or propagating material treated with the compositions described in the present document.
专利号:US-7151196-B2 优先权日:2004-11-01 标题 :Estrogen receptor modulators 发明人:WILKENING ROBERT R; FRIED AMY 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
专利号:CN-115612114-A 优先权日:2021-07-14 标 题:Method and application of copolymer film and its enzymatic self-assembly synthesis
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合成参考文献
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