CAS: 13929-35-6; Rifamycin B

该化合物是一种复杂的抗生素,它主要以其抗菌素类的功效而闻名,主要以其抗菌素类,主要是抗菌素感染的功效而闻名,主要是抗菌素肺结核,通过细菌Amycomatosis rifamycinica发酵产生,该化合物具有独特的红外色,以其大型,多环结构为特征,其中包括一个环球岩芯和一个糖味.RNA合成细菌的功能是RNA B,具体针对依赖DNA的RNA聚合酶,它扰乱了易感染细菌的转录过程.这一行动机制使它成为治疗肺结核和其他子细胞感染的有价值的治疗剂.此外,还研究它是否可用于治疗其他细菌感染,并表明它的活动是针对某些抗菌性细菌的活动.然而,它的临床用途往往受到抗药性的发展和提供更有效的衍生物(如Rifampicin)的限制.总的来说,Rifamycin B仍然是抗菌疗法领域的一个重要化合物.

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D-Glucose rifamycin S rifamycin SVrifamycin S rifamycin O rifamycin SV Rifamycin-B-pyrrolidid

合成工艺路线路线简述

    📜利福霉素置于cytochrome P450 Enzyme Rif16,Ferredoxin Reductasese Fdr,Ferredoxin Sefdx,Transketolase Rif15,3-[(4-氨基-2-甲基-5-嘧啶基)甲基]-4-甲基-5-[4,6,6-三羟基-4,6-二氧-3,5-二氧-4,6-二磷(五)己-1-基]噻唑-3-鎓,氧气,还原型辅酶ii(Nadph)四钠盐,Magnesium Chloride体系中,用 水 用作溶剂,化学反应 8.0H,反应生成利福霉素b
    参考文献:解读利福霉素生物合成的后期步骤.
    标题:解读利福霉素生物合成的后期步骤.
    摘要:利福霉素衍生的药物,包括利福平,利福布汀,利福喷丁和利福昔明,长期以来一直被用作治疗结核病和其他致命感染的一线疗法.然而,导致工业上重要的利福霉素sv和b的生物合成的后期步骤在很大程度上仍是未知的.在这里,我们表征了利福霉素sv,S,L,O和b生物合成基础的反应网络.发现两个亚基转酮酶rif15和细胞色素p450酶rif16分别介导利福霉素中独特的co键形成l和从利福霉素l到b的非典型p450酯至醚的转化.这两个反应都展示了这两个广为研究的酶家族有趣的化学性质.
    Doi:10.1038/s41467-018-04772-X

    海关参考信息

    专利信息


    专利号:US-4557866-A
    优先权日:1984-05-15
    标 题 :Process for the synthesis of pyrido-imidazo rifamycins
    发明人:CANNATA VINCENZO; TAMAGNONE GIAN F
    权利人:ALFA FARMACEUTICI SPA
    摘要:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1-4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin O of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before.

    专利号:US-2002192767-A1
    优先权日:1999-10-13
    标题 :Biosynthesis of polyketide synthase substrates
    发明人:KHOSLA CHAITAN; PFEIFER BLAINE
    摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. coli . Production can be enhanced in microbial organisms of polyketides and other secondary metabolites by delaying production until after exponential phase and by maintaining relatively constant nutrient levels in the medium. In addition, polyketide production can be enhanced by providing an expression system for a thioesterase II. Thus, by modifying the host organism and changing the culture conditions, synthesis of a secondary metabolite can be enhanced. The present invention also results in a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.

    专利号:WO-02068613-A1
    优先权日:2001-02-28
    标题 :Biosynthesis of polyketide synthase substrates
    发明人:KHOSLA CHAITAN; PFEIFER BLAINE
    权利人:UNIV LELAND STANFORD JUNIOR; KHOSLA CHAITAN; PFEIFER BLAINE
    摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. coli. Production can be enhanced in microbial organisms of polyketides and other secondary metabolites by delaying production until after exponential phase and by maintaining relatively constant nutrient levels in the medium. In addition, polyketide production can be enhanced by providing an expression system for a thioesterase II. Thus, by modifying the host organism and changing the culture conditions, synthesis of a secondary metabolite can be enhanced. The present invention also results in a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.

    专利号:US-7510852-B2
    优先权日:2002-10-18
    标题:Biosynthetic genes and host cells for the synthesis of polyketide antibiotics and method of use
    发明人:ROYER MONIQUE; GABRIEL DEAN W; FRUTOS ROGER; ROTT PHILIPPE
    权利人:CIRAD; UNIV FLORIDA
    摘要:Three gene clusters that together encode albicidin biosynthesis, the complete gene DNA sequences, and the deduced protein sequences for the enzymes and methods for using the DNA sequences are disclosed and discussed as well as methods for plant protection and creating new antibiotics. The novel Albicidin family of antibiotics is disclosed and their structure deduced.

    专利号:US-2002045220-A1
    优先权日:1999-10-13
    标题:Biosynthesis of polyketide synthase substrates
    发明人:KHOSLA CHAITAN; PFEIFER BLAINE
    摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. col. This achievement permits a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.

    专利号:US-9150590-B2
    优先权日:2011-05-19
    标 题 :Process for the synthesis of rifaximin and a new pseudo-crystalline form of rifaximin obtained thereby
    发明人:MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO
    权利人:MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO; FRIULCHEM SPA
    摘要:Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby.

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    合成参考文献


    摘要:Antibiotics Annual., 7(277), 1959/1960
    摘要:Merck Index; an Encyclopedia of Chemicals, Drugs, and Biologicals, 11th ed., Rahway, NJ 07065, Merck & Co., Inc. 1989, 11(1308), 1989
    参考文献:10.1007/bf03190014
    摘要:Mitra SK, Sundaram R, Venkataranganna MV, Gopumadhavan S. Pharmacokinetic interaction of diabecon (D-400) with rifampicin and nifedipine. European Journal of Drug Metabolism and Pharmacokinetics. 1999 Mar;24(1):79–82. doi: 10.1007/bf03190014.
    参考文献:10.1186/s12864-015-1957-7
    摘要:Shestov M, Ontañón S, Tozeren A. Encyclopedia of bacterial gene circuits whose presence or absence correlate with pathogenicity--a large-scale system analysis of decoded bacterial genomes. BMC Genomics. 2015 Oct 13;16():773.
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