CAS: 66508-53-0; Fosmidomycin

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CAS号7200-25-1 DL-精氨酸 | CAS号66508-11-0 3-( Hydroxyamin... | CAS号64-18-6 甲酸 | CAS号2258-42-6 甲乙酐 | CAS号66508-37-0 膦胺霉素钠盐

📜3-(N-甲酰基-N-羟基氨基)丙基膦酸二乙酯置于三甲基溴硅烷体系中,用 二氯甲烷,水,乙腈 作为反应溶剂,化学反应 17.0H,反应生成 膦胺霉素
参考文献:Growth Medium-Dependent Antimicrobial Activity Of Early Stage Mep Pathway Inhibitors
标题:Growth Medium-Dependent Antimicrobial Activity Of Early Stage Mep Pathway Inhibitors
摘要:细菌病原体的体内微环境通常以营养限制为特征.因此,广泛用于评估抗菌剂的传统丰富体外培养条件往往不能很好地预测体内活性,尤其是针对代谢途径的抗菌剂.赤藓醇磷酸甲酯(mep)途径是细菌病原体产生异丙肾上腺素必不可少的途径之一,但人们对生长环境对针对该途径中酶的抑制剂的抗菌特性的影响知之甚少.mep 途径的早期步骤由 1-脱氧-D-木酮糖 5-磷酸(dxp)合成酶和还原异构酶(ispc)催化.最近有报道称,Dxp 合成酶抑制剂丁乙酰基膦酸盐(bap)的体外抗菌效力与生长介质有很大关系,在营养限制条件下效力较高,而在营养丰富的条件下活性极弱.相比之下,众所周知的 Ispc 抑制剂磷霉素在营养丰富的条件下具有很强的抗菌活性,但迄今为止,还没有人在更相关的营养受限条件下探索过它的功效.这项工作的目的是彻底鉴定 Bap 和磷霉素在不同生长条件下对细菌细胞的影响.在这项工作中,我们发现这两种抑制剂的活性,无论是单独使用还是混合使用,都与生长介质密切相关,而细胞摄取量的不同也导致了两种抑制剂效力的差异.磷霉素与 Bap 不同,它在营养有限的条件下比营养丰富的条件下显示出相对较弱的活性.有趣的是,虽然人们普遍认为磷霉素的活性取决于 Glpt 转运体的表达,但我们的研究结果首次表明,磷霉素可以在营养限制条件下通过另一种机制进入细胞.最后,我们发现 Bap-Osmidomycin组合的效力和关系也取决于生长介质,揭示了在营养限制条件下 Bap-Osmidomycin协同作用的显著丧失.bap-Osmidomycin关系的这种变化表明,伴随着生长介质的变化,围绕dxp的代谢和/或调控网络也发生了变化.更广泛地说,我们的发现强调了在预测 Mep 通路抑制剂的抗菌潜力和研究其细胞内靶标时考虑生理相关生长条件的重要性.
DOI:10.1371/journal.Pone.0197638

专利信息

专利号:US-9409879-B2
优先权日:2011-03-29
标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
发明人：DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

专利号:US-10925945-B2
优先权日:2014-10-13
标题 :Bacterial vaccines deficient in the 2-C-methyl-D-erythritol-4-phosphate pathway and methods of preparation and use thereof
发明人：BAHJAT KEITH; KOGUCHI YOSHINOBU; ALICE ALEJANDRO F
权利人:PROVIDENCE HEALTH & SERVICES OREGON
摘要:The present invention relates to the preparation and use in primates of whole organismvaccines in which the MEP pathway is disrupted such that synthesis of HMBPP by the bacterial cells is substantially blocked. The data provided demonstrates that, when bacteria or other vaccine vectors that comprise an active MEP pathway are used in vaccine methods, the γδ T cell response dominates, potentially clearing the vaccine strain via γδ T cell-mediated killing of vector infected antigen presenting cells and reducing its utility as a stimulator of a productive adaptive immune response, specifically priming or boosting of CD4 + and CD8 + αβ T cell responses, specific for listerial-encoded antigens. By disrupting the MEP pathway, activation and expansion of γδ T cells is limited in the recipient primate, resulting in resulting in an increase in the magnitude and duration of inflammation and in the magnitude and duration of antigen presentation by the cellular vaccine.

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).

专利号:US-2022162188-A1
优先权日:2019-01-15
标 题:Isoprenoids and methods of making thereof
发明人：WILLIAMS GAVIN; LUND SEAN; HALL RACHAEL
权利人:UNIV NORTH CAROLINA STATE
摘要:Disclosed are methods for preparing isoprenoid subunits, as well as methods of employing these isoprenoid subunits for the synthesis of isoprenoids. Also provided are isoprenoids prepared using the methods described herein.

专利号:EP-1260590-B1
优先权日:2000-03-02
标 题 :Method of screening substance specifically inhibiting non-mevalonate pathway
发明人：SETO HARUO; KUZUYAMA TOMOHISA; MITSUI NOBUO
权利人:TOUDAI TLO LTD
摘要:The present invention provides a method for screening substances which specifically inhibit the non-mevalonate pathway by using an organism capable of using both the mevalonate pathway and the non-mevalonate pathway as biosynthetic pathways of isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). According to the present invention, it is possible to provide a novel method for screening anti-bacterial agents, herbicides or anti-malarial agents which can specifically inhibit any of the enzyme reactions on the non-mevalonate pathway for the synthesis of isopentenyl diphosphate and dimethylallyl diphosphate (DMAPP).

专利号:WO-0183769-A9
优先权日:2000-05-03
标 题 :Crystallization of 4-diphosphocytidyl-2-c-methylerythritol synthesis
发明人：NOEL JOSEPH P; BOWMAN MARIANNE E; RICHARD STEPHANE
权利人:SALK INST FOR BIOLOGICAL STUDI; NOEL JOSEPH P; BOWMAN MARIANNE E; RICHARD STEPHANE
摘要:The present invention provides the structure of the enzyme 4-diphosphocytidyl-2-C-methylerythritol (CDP-ME) synthase, a member of the cytidyltransferase family of enzymes. CDP-ME is a critical intermediate in the mevalonate-independent pathway for isoprenoid biosynthesis in a number of prokaryotic organisms, in algae, in the plastids of plants, and in the malaria parasite. Since vertebrates synthesize isoprenoid precursors using a mevalonate pathway, CDP-ME synthase and other enzymes of the mevalonate-independent pathway for isoprenoid production represent attractive targets for the structure-based design of selective antibacterial, herbicidal, and antimalarial drugs. Accordingly, the present invention provides methods for screening for compounds that inhibit enzymes of the mevalonate-independent pathway and pharmaceutical compositions and antibacterial formulations thereof. Further provided are methods of inhibiting the enzymes of the pathway and bacterial terpenoid synthesis and methods for treating a subject suffering from a bacterial infection.