CAS: 35834-26-5; Rosamicin

该化合物是一种化学化合物,被归类为大型硅酸抗生素,主要以其抗菌特性而闻名,其来源是微粒菌菌菌的具体菌株发酵,该化合物展示了针对各种抗淋病细菌的广泛活动,使其有助于治疗这些病原体造成的感染.罗沙米因功能抑制细菌蛋白合成,从而阻止细菌的生长和繁殖.其结构特征是大型乳胶环,是大型硅酸酯,是其生物活动必不可少的.该化合物通常在临床环境中施用,其药用植物基因学,包括吸收,分布,新陈代谢和排泄物,对于确定其功效和安全特征至关重要.虽然它在治疗某些感染方面已经显示出希望,但抗生素抗体的出现仍是一个令人关切的问题,需要仔细考虑其在临床实践中的用途.

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CAS号102438-11-9 rosaramicin N-oxide | CAS号61486-91-7 12,13-de-epoxy-... | CAS号122825-80-3 rosaramicin 20-... | CAS号56689-42-0 de-epoxy rosamicin | CAS号61486-91-7 12,13-de-epoxy-...

合成工艺路线路线简述

    📜(S)-2-((Benzyloxy)Methyl)Butan-1-Ol置于咪唑,N-甲基咪唑,二乙烯基砜,2,2'-联吡啶,Sodium Periodate,正丁基锂,硼烷铵络合物,Glucose-6-Phosphate Dehydrogenase,2,2,6,6-四甲基哌啶氧化物,Glucose-6-Phosphate,三丁基膦,Ruthenium(Iii) Chloride Trihydrate,Palladium 10% On Activated Carbon,Nicotinamide Adenine Dinucleotide Phosphate,氢氟酸,氢气,碘,三氟甲烷磺酸亚铜(I)苯联合体 (2:1),Sodium Hydride,Caesium Carbonate,二异丙胺,三苯基膦,Lithium Chloride体系中,用 四氢呋喃,四氯化碳,Aq. Phosphate Buffer,正己烷,二氯甲烷,水,二甲基亚砜,乙酸乙酯,N,N-二甲基甲酰胺,异丙醇,乙腈 作为反应溶剂,化学反应 170.0H,反应生成 蔷薇霉素
    参考文献:通过后期聚酮化合物组装,剪裁和 C-H 功能化实现基于泰内酯的大环内酯抗生素的化学酶促总合成和结构多样化
    标题:通过后期聚酮化合物组装,剪裁和 C-H 功能化实现基于泰内酯的大环内酯抗生素的化学酶促总合成和结构多样化
    摘要:聚酮合酶 (Pks) 是一种强大的催化平台,能够影响多个碳-碳键形成反应和氧化态调整.我们探索了产生 16 元泰乐菌素大环的两个末端 Pks 模块的功能,将它们用作泰内酯化学酶法合成中的生物催化剂,并在随后的阐述中完成了 Juvenimicin,M-4365 和 Rosamicin 类的首次全合成通过后期多样化开发大环内酯类抗生素.采用合成化学来反应生成可被倒数第二个 Juveiv Pks 模块的 Juvenimicin (Juv) 酮合酶接受的 Tylactone 六酮链延长中间体.六酮化合物在体外通过两个完整的模块(juveiv 和 Juvev)进行处理,其催化两个酮化合物单元的延伸和官能化,然后将所得八酮化合物环化成丁内酯.大环内酯化后,结合体内糖基化,选择性体外细胞色素 P450 介导的氧化和化学氧化,以少至 15 个线性步骤(总共 21 个)完成一系列大环内酯天然产物的可扩展构建.产率为
    DOI:10.1021/jacs.7B02875

    海关参考信息

    专利信息


    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:US-6667406-B1
    优先权日:1999-03-10
    标题 :Methods for the synthesis of complex reduced isoindole, isooxyindole and isooxyquinoline libraries
    发明人:SUN SENGEN; MURRAY WILLIAM V
    权利人:ORTHO MCNEIL PHARM INC
    摘要:Disclosed are methods of synthesizing libraries of diverse complex hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds through the use of a facile intramolecular Diels Alder reaction. The invention is further directed to methods for synthesizing the libraries on solid supports. The invention is further directed to methods for identifying and isolating such hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds with useful and diverse activities from such libraries.

    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-9907753-B2
    优先权日:2010-03-19
    标 题 :Lipid vesicle compositions and methods of use
    发明人:IRVINE DARRELL J; MOON JAEHYUN
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

    专利号:US-8933018-B2
    优先权日:2011-02-07
    标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
    发明人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA
    权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC
    摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Massa T, Davis GJ, Schiavo D, Sinha DP, Szot RJ, Black HE, Schwartz E. Tapetal changes in beagle dogs. II. Ocular changes after intravenous administration of a macrolide antibiotic--rosaramicin. Toxicol Appl Pharmacol. 1984 Feb;72(2):195-200.
    4: Robson HG, Shah PP, Lalonde RG, Hayes L, Senikas VM. Comparison of rosaramicin and erythromycin stearate for treatment of cervical infection with Chlamydia trachomatis. Sex Transm Dis. 1983 Jul-Sep;10(3):130-4.
    6: Lin CC, Kim HK, Marco A, Radwanski E, Symchowicz S. Pharmacokinetics and metabolism of [14C]rosaramicin in dogs. Antimicrob Agents Chemother. 1986 May;29(5):753-6.

    合成参考文献


    摘要:Journal of Antibiotics., 25(647), 1972 []
    摘要:Journal of Antibiotics., 25(641), 1972 []
    摘要:Journal of Antibiotics., 43(938), 1990 []
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