Synthesis of Hydrophobic N'-Mono and N',N'-Double Alkylated Eremomycins Inhibiting the Transglycosylation Stage of Bacterial Cell Wal Biosynthesis

A.Y.Pavlov; O.V.Miroshinikova; S.S.Printsevskaya; E.N.Olsufyeva; M.N.Preobrazhenskaya; R.C.Goldman; A.A.Branstrom; E.R.Baizman; C.B.Longley

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Synthesis of Hydrophobic N'-Mono and N',N'-Double Alkylated Eremomycins Inhibiting the Transglycosylation Stage of Bacterial Cell Wal Biosynthesis

机译：疏水性N'-Mono和N'，N“-双烷基化emeromycins抑制细菌Wal生物合成的转糖基化阶段的合成。

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A series of hydrophobic N'-mono and N',N"-doubl ealkylated derivatives of the glycopeptide antibiotic eremomycin were synthesized by reductive alkylation after preliminary protectionof the N-terminal amino group of the peptide backbone.The investigation of the antibacterial activity in vitro showed that N'=C_(10)H_(21)- and N'-p-(p-chlorophenyl)benzyl derivatives of eremomycin are the most active against vancomycin-resistant enterococci among the compounds obtained though they are less effective than the corresponding lipophilic derivatives of vancomycin.The introduction of two hydrophobic substituents led to a decrease in activity against both susecptible and resistant bacteria.The biochemical evaluation of the mode of action revealed that in addition to binding to D-Ala-D-Ala these compounds also have an alternative mechanism of action the does not require substrate binding.

机译：在初步保护肽主链N端氨基后，通过还原烷基化反应，合成了一系列糖肽抗生素埃雷霉素的疏水性N'-单和N'，N“-双烷基化烷基化衍生物。体外抗菌活性的研究结果表明，在获得的化合物中，埃雷霉素的N'= C_（10）H_（21）-和N'-对-（对氯苯基）苄基衍生物对耐万古霉素肠球菌的活性最高，但效果不如相应化合物。万古霉素的亲脂性衍生物。两个疏水取代基的引入导致针对可疑细菌和耐药细菌的活性降低。作用方式的生化评估表明，除与D-Ala-D-Ala结合外，这些化合物还具有另一种作用机理是不需要底物结合。

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《The Journal of Antibiotics: An International Journal》 |2001年第5期|共5页
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A.Y.Pavlov; O.V.Miroshinikova; S.S.Printsevskaya; E.N.Olsufyeva; M.N.Preobrazhenskaya; R.C.Goldman; A.A.Branstrom; E.R.Baizman; C.B.Longley;
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正文语种 eng
中图分类药学;药品;
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1. Synthesis of Hydrophobic N'-Mono and N',N"-Double Alkylated Eremomycins Inhibiting the Transglycosylation Stage of Bacterial Cell Wal Biosynthesis [J] . A.Y.Pavlov, O.V.Miroshinikova, S.S.Printsevskaya, The Journal of Antibiotics: An International Journal . 2001,第5期

机译：疏水性N'-Mono和N'，N“-双烷基化emeromycins抑制细菌Wal生物合成的转糖基化阶段的合成。
2. Treatment with inhibitors of polyamine biosynthesis, which selectively lower intracellular spermine, does not affect the activity of alkylating agents but antagonizes the cytotoxicity of DNA topoisomerase II inhibitors [J] . MA Desiderio, D Bergamaschi, E Mascellani, British Journal of Cancer . 1997,第7期

机译：用多胺生物合成抑制剂处理（选择性降低细胞内精胺）不会影响烷基化剂的活性，但会拮抗DNA拓扑异构酶II抑制剂的细胞毒性。
3. Synthesis and mode of action of hydrophobic derivatives of the glycopeptide antibiotic eremomycin and des-(N-methyl-D-leucyl)eremomycin against glycopeptide-sensitive and -resistant bacteria. [J] . Printsevskaya SvetlanaS, Pavlov AndreyY, Olsufyeva EvgeniaN, Journal of Medicinal Chemistry . 2002,第6期

机译：糖肽抗生素埃雷霉素和去-（N-甲基-D-亮氨酰）埃雷霉素疏水衍生物对糖肽敏感和耐药细菌的合成和作用方式。
4. Biosynthesis of Polyhydroxyalkanoates from 4-Ketovaleric Acid in Bacterial Cells [C] . Jian Yu Symposium on green polymer chemistry . 2010

机译：细菌细胞4-酮戊酸聚羟基烷烃的生物合成
5. Mechanistic Studies of Novel Inhibitors Targeting the Bacterial Menaquinone Biosynthesis Pathway. [D] . Matarlo, Joe Sumagang. 2016

机译：针对细菌甲萘醌生物合成途径的新型抑制剂的机理研究。
6. Oxaziclomefone a New Herbicide Inhibits Wall Expansion in Maize Cell-cultures without Affecting Polysaccharide Biosynthesis Xyloglucan Transglycosylation Peroxidase Action or Apoplastic Ascorbate Oxidation [O] . NICHOLA OLOONEY, STEPHEN C. FRY 2005

机译：恶唑烷酮是一种新型除草剂可在不影响多糖生物合成木葡聚糖转糖基化过氧化物酶作用或质外抗坏血酸氧化的情况下抑制玉米细胞培养中的壁膨胀。
7. Treatment with inhibitors of polyamine biosynthesis, which selectively lower intracellular spermine, does not affect the activity of alkylating agents but antagonizes the cytotoxicity of DNA topoisomerase II inhibitors. [O] . Desiderio, M. A., Bergamaschi, D., Mascellani, E., 1997

机译：用多胺生物合成抑制剂（选择性降低细胞内精胺）的处理不会影响烷基化剂的活性，但会拮抗DNA拓扑异构酶II抑制剂的细胞毒性。

Synthesis of Hydrophobic N'-Mono and N',N'-Double Alkylated Eremomycins Inhibiting the Transglycosylation Stage of Bacterial Cell Wal Biosynthesis

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