دورية أكاديمية

[Design of Novel Carboxamides of Eremomycin and Vancomycin with 4- or 3-Amino Methyl Phenyl Boric Acid and Their Investigation].

التفاصيل البيبلوغرافية
العنوان: [Design of Novel Carboxamides of Eremomycin and Vancomycin with 4- or 3-Amino Methyl Phenyl Boric Acid and Their Investigation].
المؤلفون: Bychkova EN, Korolev AM, Olsufyeva EN, Mirchink EP, Isakova EB
المصدر: Antibiotiki i khimioterapiia = Antibiotics and chemoterapy [sic] [Antibiot Khimioter] 2015; Vol. 60 (9-10), pp. 7-11.
نوع المنشور: English Abstract; Journal Article; Research Support, Non-U.S. Gov't
اللغة: Russian
بيانات الدورية: Publisher: Izdatelstvo Meditsina Country of Publication: Russia (Federation) NLM ID: 8803688 Publication Model: Print Cited Medium: Print ISSN: 0235-2990 (Print) Linking ISSN: 02352990 NLM ISO Abbreviation: Antibiot Khimioter Subsets: MEDLINE
أسماء مطبوعة: Publication: Moskva : Izdatelstvo Meditsina
Original Publication: Moskva : Meditsina, c1988-
مواضيع طبية MeSH: Drug Design*, Anti-Bacterial Agents/*chemical synthesis , Boronic Acids/*chemistry , Glycopeptides/*chemical synthesis , Gram-Positive Bacteria/*drug effects , Vancomycin/*analogs & derivatives , Vancomycin/*chemical synthesis, Anti-Bacterial Agents/chemistry ; Dose-Response Relationship, Drug ; Glycopeptides/chemistry ; Microbial Sensitivity Tests ; Molecular Structure ; Vancomycin/chemistry
مستخلص: Amidation of the end carboxyl group of eremomycin and vancomycin by pinacolinic 4- or 3-amino methyl phenyl boron acids esters in the presence of the condensing reagent PyBOP resulted in formation of novel carboxamides of the antibiotics (IIIa-VIa). After elimination of the pinacolinic group under mild hydrolysis in weak acid aqueous medium there formed the respective derivatives with a residue of the nonprotected boric acid (III-VI). It was shown that the activity of the 4-substituted derivatives of the borole-containing eremomycin and vancomycin practically was the same as that of the initial antibiotics, while higher than that of the respective 3-substituted derivatives of the borole-containing derivatives against 8 strains of grampositive bacteria.
المشرفين على المادة: 0 (Anti-Bacterial Agents)
0 (Boronic Acids)
0 (Glycopeptides)
110865-90-2 (eremomycin)
6Q205EH1VU (Vancomycin)
تواريخ الأحداث: Date Created: 20160505 Date Completed: 20160609 Latest Revision: 20161020
رمز التحديث: 20221213
PMID: 27141632
قاعدة البيانات: MEDLINE