CAS: 68-35-9; Sulfadiazine

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4-硝基-N-2-嘧啶基-苯磺酰胺置于palladium 10% On Activated Carbon体系中,用 四氢呋喃,甲醇,乙酸乙酯 作为反应溶剂,50.0 °C,5.0 Mpa 条件下,反应生成 磺胺嘧啶
参考文献:4-((2-羟基-3-甲氧基苄基)氨基)苯磺酰胺衍生物作为 12-脂氧化酶的强效和选择性抑制剂的合成和构效关系研究
标题:4-((2-羟基-3-甲氧基苄基)氨基)苯磺酰胺衍生物作为 12-脂氧化酶的强效和选择性抑制剂的合成和构效关系研究
摘要:人类脂肪氧化酶 (Lox) 是一类含铁酶,可催化多不饱和脂肪酸氧化以提供相应的生物活性羟基二十碳四烯酸 (Hete) 代谢物.这些类二十烷酸信号分子参与了许多生理反应,例如血小板聚集,炎症和细胞增殖.我们小组对血小板型 12-(S)-Lox (12-Lox)产生了特别的兴趣,因为它在皮肤病,糖尿病,血小板止血,血栓形成和癌症中发挥了重要作用.在此,我们报告了基于 4-((2-羟基-3-甲氧基苄基)氨基)苯磺酰胺的支架的鉴定和药物化学优化.顶级化合物,以35和36为例,显示对 12-Lox 的 Nm 效力,对相关脂肪氧化酶和环氧化酶具有出色的选择性,并具有非常好的 Adme 特性.此外,这两种化合物均抑制 Par-4 诱导的人血小板聚集和钙动员,并减少 β 细胞中的 12-Hete.
DOI:10.1021/jm4016476

专利信息

专利号:US-5442065-A
优先权日:1993-09-09
标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin
发明人：MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A
权利人:UNIV TEXAS
摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.

专利号:US-10768157-B2
优先权日:2015-10-20
标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples
发明人：KABIR ABUZAR; FURTON KENNETH G
权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.

专利号:US-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:EP-2690438-A1
优先权日:2012-07-24
标题:Synthesis of diverse glycosylphosphatidylinositol glycans and glycolipids from toxoplasma gondii and their application as diagnostic markers and vaccines
发明人：AZZOUZ NAHID; GOETZE SEBASTIAN; SEEBERGER PETER H; SILVA DANIEL VARON; TSAI YU-HSUAN
权利人:MAX PLANCK GESELLSCHAFT
摘要:The present invention relates to the synthesis of compounds derived from glycosylphosphatidylinositol (GPI) glycolipids from Toxoplasma gondii and the resulting products obtained. These synthetic compounds are suitable for diagnosis of toxoplasmosis and for use as a vaccine against diseases caused by infection with T. gondii.

专利号:US-9802974-B2
优先权日:2012-07-24
标 题 :Synthesis of diverse glycosylphosphatidylinositol glycans from Toxoplasma gondii and their application as vaccines and diagnostics
发明人：AZZOUZ NAHID; GÖTZE SEBASTIAN; SEEBERGER PETER H; SILVA DANIEL VARON; TSAI YU-HSUAN
权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V
摘要:The present invention relates to the synthesis of GPI-related surface antigens of the parasite Toxoplasma gondii ( T. gondii ) and the resulting products obtained. These synthetic compounds are suitable for diagnosis of toxoplasmosis, as well as vaccine against toxoplasmosis, a diseases caused by infection with T. gondii.

专利号:US-10308663-B2
优先权日:2015-06-16
标题:Inhibitors of PTP4A3 for the treatment of cancer
发明人：LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M
权利人:LAZO JOHN S; SHARLOW ELIZABETH R; MCQUEENEY KELLEY E; WIPF PETER; SALAMOUN JOSEPH M; UNIV VIRGINIA PATENT FOUNDATION; UNIV OF PITTSBURGH —OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
摘要:The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).