CAS: 38129-37-2; Bicozamycin

该化合物是一种属于百草枯类的广泛的抗生素,主要对抗克菌阳性细菌和某些克菌阴性细菌有效,其行动机制包括抑制细菌细胞壁合成,使其在抗抗药菌株方面特别有用;该化合物具有低毒性和有利的药源特性,确保治疗应用的稳定性和生物利用率;Bicozamycin通常用于兽医治疗牲畜肠胃感染,因为其残留效应和效力极小;它针对病原细菌的选择性活动,同时保留有益的微生物,进一步增强其在动物健康的效用;该抗生素与其他抗微生物剂的兼容性,允许混合疗法.

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CAS号114533-59-4 4-hydroxy-3-(2-... | CAS号114533-60-7 3,4-dihydroxy-5... | CAS号37134-40-0 苯甲酸双环霉素 | CAS号41238-48-6 1-hydroxy-2-met...

合成工艺路线路线简述

  • 合成目标产物 Bicozamycin 主要起始原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
  • (文献来源)合成步骤主要原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy-
📜(1S,6R)-6-<(Tert-Butyldimethylsilyl)Oxy>-1-<(1S,2S)-2,3-Dihydroxy-2,3-O-Isopropylidene-1-(P-Methoxybenzyl)-2-Methylpropyl>-7,9-Bis(P-Methoxybenzyl)-5-Methylene-7,9-Diaza-2-Oxabicyclo<4.2.2>Decane-8,10-Dione置于ammonium Cerium(Iv) Nitrate,四丁基氟化铵,水,2,3-二氯-5,6-二氰基-1,4-苯醌体系中,用 四氢呋喃,二氯甲烷,乙腈 作为反应溶剂,化学反应 2.92H,反应生成 二环霉素
参考文献:Chiral Synthesis Of Bicyclomycin And Diastereomeric Stereoselectivity Of The Key Aldol Condensation
标题:Chiral Synthesis Of Bicyclomycin And Diastereomeric Stereoselectivity Of The Key Aldol Condensation
摘要:
DOI:10.1021/jo00261A009

海关参考信息

专利信息


专利号:US-7723082-B2
优先权日:2002-06-21
标题 :Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives
发明人:GONDRY MURIEL; GENET ROGER; LAUTRU SYLVIE; PERNODET JEAN-LUC
权利人:COMMISSARIAT ENERGIE ATOMIQUE; CENTRE NAT RECH SCIENT
摘要:The invention concerns novel isolated natural or synthetic polynucleotides and polypeptides coded by said polynucleotides, involved in the synthesis of diketopiperazine derivatives, vectors comprising said polynucleotides, micro-organisms transformed with said polynucleotides, uses of said polynucleotides and said polypeptides, as well as methods for the synthesis of diketopiperazine derivatives, including cyclodipeptides and diketopiperazine derivatives 3- and 6-substituted by α,β-unsaturated amino acid side chains.

专利号:US-5817751-A
优先权日:1994-06-23
标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives
发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID
权利人:AFFYMAX TECH NV
摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.

专利号:WO-9600391-A1
优先权日:1994-06-23
标题:Methods for the synthesis of diketopiperazines
发明人:CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.

专利号:US-2006051837-A1
优先权日:2002-06-21
标 题 :Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives

专利号:US-2021163451-A1
优先权日:2018-05-16
标题:Methods and compositions for substituted 2,5-diketopiperazine analogs
发明人:DING YOUSONG; JIANG GUANGDE
权利人:UNIV FLORIDA
摘要:Thaxtomins are phytotoxic secondary metabolites produced in plant pathogenic Streptomyces strains and have received considerable interests as bioherbicides. A cell-free, biocombinatorial approach was developed to produce a thaxtomin library for herbicide development. Combination of biosynthetic enzymes led to the production of 136 substituted 2,5-diketopiperazines, thaxtomin D, thaxtomin B and thaxtomin A analogs in a single pot. Furthermore, rational engineering of TxtA allowed the synthesis of azido-containing thaxtomin analog. Selected unnatural thaxtomins demonstrated improved herbicidal activities. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

专利号:US-2007048817-A1
优先权日:2002-06-21
标 题:Polynucleotides and polypeptides coded by said polynucleotides involved in the synthesis of diketopiperazine derivatives

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主要参考文献


1: Tran L, van Baarsel JA, Washburn RS, Gottesman ME, Miller JH. Single-gene deletion mutants of Escherichia coli with altered sensitivity to bicyclomycin, an inhibitor of transcription termination factor Rho. J Bacteriol. 2011 May;193(9):2229-35. doi: 10.1128/JB.01463-10. Epub 2011 Feb 25.
2: Weber TP, Widger WR, Kohn H. The Mg2+ requirements for rho transcription termination factor: catalysis and bicyclomycin inhibition. Biochemistry. 2002 Oct 15;41(41):12377-83. doi: 10.1111/febs.13226. Epub 2015 Feb 27. doi: 10.1093/jac/dku285. Epub 2014 Jul 31.
7: Santillán A Jr, Zhang X, Hardesty J, Widger WR, Kohn H. Role of the C(6)-hydroxy group in bicyclomycin: synthesis, structure, and chemical, biochemical, and biological properties. J Med Chem. 1998 Mar 26;41(7):1185-94. Epub 2003 Jan 27.

合成参考文献


摘要:Journal of Antibiotics., 25(569), 1972 []
参考文献:10.1007/s001080050448
摘要:Kollaritsch H. [Travellers' diarrhea]. Internist (Berl). 1999 Nov;40(11):1132–6. doi: 10.1007/s001080050448.
参考文献:10.1007/s101560200022
摘要:Kumazawa J, Yagisawa M. The history of antibiotics: the Japanese story. J Infect Chemother. 2002 Jun;8(2):125–33. doi: 10.1007/s101560200022.
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