CAS: 112362-50-2; (3R,4R,5E,10E,12E,14S,26R,26As)-26-[[2-(Diethylamino)Ethyl]Sulfonyl]-8,9,14,15,24,25,26,26A-Octahydro-14-Hydroxy-4,12-Dimethyl-3-(1-Methylethyl)-3H-21,18-Nitrilo-1H,22H-Pyrrolo[2,1-C][1,8,4,19]Dioxadiazacyclotetracosine-1,7,16,22(4H,17H)-Tetrone

该化合物是二AA 的半合成合成抗生素. 它通过与50S 脊髓膜炎分管结合,具体针对peptidyl转移酶中心,作为抗甲状腺素的抗菌素. Dalfopristin 主要是与五氯苯丙胺(作为合成体)结合,用于治疗严重的青蒿素性感染,包括抗甲状腺素(MRSA)和抗氯素(抗肠胃炎)法属菌(VRE)引起的感染.它的协同机制可以加强细菌灭菌活动,降低抗药性发展的可能性. 化合物展示了有利的致癌性,包括组织渗透,并且通过静脉注射方式进行. 它的临床效用因它对抗多抗药病原体而得到强调.

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    专利信息


    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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:US-10899773-B2
    优先权日:2014-12-19
    标 题 :Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs
    发明人:NICOLAOU KYRIACOS C; CAI QUAN
    权利人:UNIV RICE WILLIAM M
    摘要:In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.

    专利号:US-2016185745-A1
    优先权日:2013-08-07
    标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
    发明人:SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
    权利人:UNIV TEXAS
    摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    专利号:US-9382288-B2
    优先权日:2010-10-06
    标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
    发明人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
    权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
    摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

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    主要参考文献


    1: Maraki S, Samonis G, Dimopoulou D, Mantadakis E. Susceptibility of Glycopeptide-Resistant Enterococci to Linezolid, Quinupristin/dalfopristin, Tigecycline and Daptomycin in a Tertiary Greek Hospital. Infect Chemother. 2014 Dec;46(4):253-6. doi: 10.3947/ic.2014.46.4.253. Epub 2014 Dec 29.
    2: Yu F, Lu C, Liu Y, Sun H, Shang Y, Ding Y, Li D, Qin Z, Parsons C, Huang X, Li Y, Hu L, Wang L. Emergence of quinupristin/dalfopristin resistance among livestock-associated Staphylococcus aureus ST9 clinical isolates. Int J Antimicrob Agents. 2014 Nov;44(5):416-9. doi: 10.1016/j.ijantimicag.2014.06.020. Epub 2014 Aug 17. doi: 10.3967/bes2014.065. doi: 10.4103/0377-4929.116164. doi: 10.1089/mdr.2012.0176. Epub 2013 Feb 26. doi: 10.1001/archophthalmol.2012.1504. doi: 10.1016/j.mcna.2011.03.011. doi: 10.1186/1752-1947-5-130.
    9: Bhatawadekar S, Chattopadhyay A. Quinpristin-Dalfopristin resistance among methicillin-resistant strains of staphylococci. Indian J Pharmacol. 2010 Feb;42(1):56. doi: 10.4103/0253-7613.62403.

    合成参考文献


    参考文献:10.1007/s00431-011-1520-8
    摘要:Knirsch W, Nadal D. Infective endocarditis in congenital heart disease. European Journal of Pediatrics. 2011 Jul 20;170(9):1111. doi: 10.1007/s00431-011-1520-8.
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