📜6-氨基青霉烷酸,六氢-1-(甲氧基亚甲基)-1H-氮杂卓鎓硫酸甲酯盐置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 美西林 参考文献:Studies On Prodrugs. Vi Preparation And Characterization Of (5-Substituted 2-Oxo-1,3-Dioxol-4-yl)Methyl Esters Of Mecillinam. 标题:Studies On Prodrugs. Vi Preparation And Characterization Of (5-Substituted 2-Oxo-1,3-Dioxol-4-yl)Methyl Esters Of Mecillinam. 摘要:作为一种新型甲氧西林原药,我们制备了甲氧西林(5-取代的 2-氧代-1,3-二氧戊环-4-基)甲酯.研究发现,小鼠口服这些酯类药物后,血液中的美西林含量至少是美西林本身的 4 倍.美西林(5-甲基-2-氧代-1,3-二氧戊环-4-基)甲酯盐酸盐具有吸湿性,但其 L-酒石酸盐不具有吸湿性. DOI:10.1248/cpb.35.642
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-9868747-B2 优先权日:2014-02-18 标题:Marinopyrrole derivatives and methods of making and using same 发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI 权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD 摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
专利号:US-2025002508-A1 优先权日:2020-05-05 标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof 发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS 权利人:QPEX BIOPHARMA INC 摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
专利号:CN-109371095-A 优先权日:2018-12-06 标题 :A kind of method of enzymatic synthesis of amoxicillin
专利号:US-4452796-A 优先权日:1982-06-14 标题:6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors 发明人:BARTH WAYNE E 权利人:PFIZER 摘要:Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.
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合成参考文献
参考文献:10.1046/j.1469-0691.2002.00376.x 摘要:Bruun B, Gahrn-Hansen B. Mecillinam susceptibility as an indicator of beta-lactamase production in Staphylococcus aureus. Clin Microbiol Infect. 2002 Feb;8(2):122–4. doi: 10.1046/j.1469-0691.2002.00376.x. 参考文献:10.1093/jac/dkh233 摘要:Bostock JM, Geary I, Eley A, Chopra I. Mecillinam has potent in vitro activity against Chlamydophila pneumoniae ATCC VR1310. J Antimicrob Chemother. 2004 Jun;53(6):1112. doi: 10.1093/jac/dkh233. 参考文献:10.1007/978-1-4939-2854-5_1 摘要:Verstraeten N, Knapen W, Fauvart M, Michiels J. A Historical Perspective on Bacterial Persistence. Methods Mol Biol. 2016;1333():3–13. doi: 10.1007/978-1-4939-2854-5_1. 参考文献:10.1016/j.ijantimicag.2016.11.021 摘要:Zayyad H, Eliakim-Raz N, Leibovici L, Paul M. Revival of old antibiotics: needs, the state of evidence and expectations. International Journal of Antimicrobial Agents. 2017 May;49(5):536–41. doi: 10.1016/j.ijantimicag.2016.11.021.