CAS: 526-02-3; (E)-4-((4-Cyanobenzylidene)Amino)Benzenesulfonamide

该化合物是属于管道衍生物类的合成化合物,具有用二氯酮混合物替代的管状环,有助于其反应和潜在的生物活动;水氧和二甲基苯基组的存在表明,它可能表现出与生物目标的有趣互动,有可能影响其药用特性;该化合物经常因其在医药化学方面的应用,特别是在药品的开发方面应用而受到研究;其结构特征表明,它可能参与氢结合和其他分子间相互作用,这可能会影响其溶解性和稳定性;此外,二氯酮功能组的存在可能允许进一步的化学改变,提高它在各种化学合成物或药物发现中作为铅化合物的用途.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜放线菌酮置于n-溴代丁二酰亚胺(Nbs)体系中,用 四氯化碳 作为反应溶剂,以10%的收率获得产物4-[2-(2-羟基-3,5-二甲基苯基)-2-氧代乙基]哌啶-2,6-二酮
    参考文献:戊二酰亚胺抗生素actiketal的合成
    标题:戊二酰亚胺抗生素actiketal的合成
    摘要:Actiketal(rk-441S)的第一个合成物,一种来自链霉菌亚种的抗生素.通过关键的钯辅助偶联反应,由5,7-二甲基苯并呋喃和戊二酸二甲酯获得了epiderstagenes.
    DOI:10.1016/s0040-4039(00)00928-X

    海关参考信息

    专利信息


    专利号:US-8912150-B2
    优先权日:2001-08-03
    标题:Ribosome structure and protein synthesis inhibitors
    发明人:STEITZ THOMAS A; MOORE PETER B; SUTCLIFFE JOYCE A; OYELERE ADEGBOYEGA K; IPPOLITO JOSEPH A
    权利人:RIB X PHARMACEUTICALS INC; UNIV YALE; MELINTA THERAPEUTICS INC
    摘要:The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.

    专利号:US-6947844-B2
    优先权日:2000-08-09
    标 题 :Modulators of ribosomal function and identification thereof
    发明人:STEITZ THOMAS A; MOORE PETER B; BAN NENAD; NISSEN POUL; HANSEN JEFFREY
    权利人:UNIV YALE
    摘要:The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.

    专利号:US-6952650-B2
    优先权日:2001-08-03
    标题:Modulators of ribosomal function and identification thereof
    发明人:STEITZ THOMAS A; MOORE PETER B; BAN NENAD; NISSEN POUL; HANSEN JEFFREY
    权利人:UNIV YALE
    摘要:The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.

    专利号:EP-1188769-A2
    优先权日:2000-08-09
    标 题 :High resolution crystal structure of the ribosome and design of protein synthesis inhibitors

    专利号:EP-1188769-B1
    优先权日:2000-08-09
    标题 :High resolution crystal structure of the ribosome and design of protein synthesis inhibitors

    专利号:DE-60119853-T2
    优先权日:2000-08-09
    标题 :Crystal structure of ribosomes and protein synthesis inhibitors

    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: Yin M, Yan Y, Lohman JR, Huang SX, Ma M, Zhao GR, Xu LH, Xiang W, Shen B. Cycloheximide and actiphenol production in Streptomyces sp. YIM56141 governed by single biosynthetic machinery featuring an acyltransferase-less type I polyketide synthase. Org Lett. 2014 Jun 6;16(11):3072-5. doi: 10.1021/ol501179w. Epub 2014 May 9.
    2: Hu JQ, Zhang A, Wang H, Niu L, Wang QX, Zhu LL, Li YZ, Wu C. Discovery and Biosynthesis of Glycosylated Cycloheximide from a Millipede-Associated Actinomycete. J Nat Prod. 2023 Feb 24;86(2):340-345. doi: 10.1021/acs.jnatprod.2c00951. Epub 2023 Jan 24. 23(23):15045. doi: 10.3390/ijms232315045.
    4: Spízek J, Málek I, Suchý J, Vondrácek M, Vanĕk Z. Metabolites of Streptomyces noursei. V. Relation of the production of cycloheximide and actiphenol to the production of fungicidin. Folia Microbiol (Praha). 1965 Sep;10(5):263-6. doi: 10.1007/BF02871023. 108(2):391-402. doi: 10.1007/s10482-015-0492-5. Epub 2015 Jun 4. 28(19):1602-6. doi: 10.1080/14786419.2014.928877. Epub 2014 Jun 20.

    合成参考文献


    参考文献:10.1007/978-981-97-5165-5_21
    摘要:Harsha, Kumar M, Kumar P, Solanki R, Kapur MK. Bioactive Potential of Streptomyces Spp. Against Diverse Pathogenic Fungi. 2024. In: Advances in Antifungal Drug Development.
    参考文献:10.1007/bf02869842|10.1007/bf02871022|10.1007/bf02871023
    摘要:Spízek J, Málek I, Suchý J, Vondrácek M, Vanĕk Z. Metabolites of Streptomyces noursei. V. Relation of the production of cycloheximide and actiphenol to the production of fungicidin. Folia Microbiol (Praha). 1965 Sep;10(5):263–6. doi: 10.1007/bf02871023.
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