Novel 5′-Norcarbocyclic Pyrimidine Derivatives as Antibacterial Agents

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dc.contributor.authorKhandazhinskaya, Anastasia L.
dc.contributor.authorAlexandrova, Liudmila A.
dc.contributor.authorMatyugina, Elena S.
dc.contributor.authorSolyev, Pavel N.
dc.contributor.authorEfremenkova, Olga V.
dc.contributor.authorBuckheit, Karen W.
dc.contributor.authorWilkinson, Maggie
dc.contributor.authorBuckheit, Robert W.
dc.contributor.authorChernousova, Larisa N.
dc.contributor.authorSmirnova, Tatiana G.
dc.contributor.authorAndreevskaya, Sofya N.
dc.contributor.authorLeonova, Olga G.
dc.contributor.authorPopenko, Vladimir I.
dc.contributor.authorKochetkov, Sergey N.
dc.contributor.authorSeley-Radtke, Katherine
dc.date.accessioned2018-12-04T16:40:32Z
dc.date.available2018-12-04T16:40:32Z
dc.date.issued2018-11-23
dc.description.abstractA series of novel 5′-norcarbocyclic derivatives of 5-alkoxymethyl or 5-alkyltriazolyl-methyl uracil were synthesized and the activity of the compounds evaluated against both Gram-positive and Gram-negative bacteria. The growth of Mycobacterium smegmatis was completely inhibited by the most active compounds at a MIC99 of 67 μg/mL (mc2155) and a MIC99 of 6.7–67 μg/mL (VKPM Ac 1339). Several compounds also showed the ability to inhibit the growth of attenuated strains of Mycobacterium tuberculosis ATCC 25177 (MIC99 28–61 μg/mL) and Mycobacterium bovis ATCC 35737 (MIC99 50–60 μg/mL), as well as two virulent strains of M. tuberculosis; a laboratory strain H37Rv (MIC99 20–50 μg/mL) and a clinical strain with multiple drug resistance MS-115 (MIC99 20–50 μg/mL). Transmission electron microscopy (TEM) evaluation of M. tuberculosis H37Rv bacterial cells treated with one of the compounds demonstrated destruction of the bacterial cell wall, suggesting that the mechanism of action for these compounds may be related to their interactions with bacteria cell walls.en_US
dc.description.sponsorshipThe work was supported by Russian Science Foundation, project No 14-50-00060.en_US
dc.description.urihttps://www.mdpi.com/1420-3049/23/12/3069en_US
dc.format.extent18 pagesen_US
dc.genrejournal articlesen_US
dc.identifierdoi:10.13016/M2QR4NV48
dc.identifier.citationAnastasia L. Khandazhinskaya , Liudmila A. Alexandrova , Elena S. Matyugina, Pavel N. Solyev , Olga V. Efremenkova , Karen W. Buckheit , Maggie Wilkinson , Robert W. Buckheit, Jr. , Larisa N. Chernousova , Tatiana G. Smirnova , Sofya N. Andreevskaya , Olga G. Leonova , Vladimir I. Popenko , Sergey N. Kochetkov and Katherine L. Seley-Radtke , Novel 5′-Norcarbocyclic Pyrimidine Derivatives as Antibacterial Agents, Molecules 2018, 23(12), 3069; https://doi.org/10.3390/molecules23123069en_US
dc.identifier.urihttps://doi.org/10.3390/molecules23123069
dc.identifier.urihttp://hdl.handle.net/11603/12163
dc.language.isoen_USen_US
dc.publisherMDPIen_US
dc.relation.isAvailableAtThe University of Maryland, Baltimore County (UMBC)
dc.relation.ispartofUMBC Chemistry & Biochemistry Department Collection
dc.rightsThis item is likely protected under Title 17 of the U.S. Copyright Law. Unless on a Creative Commons license, for uses protected by Copyright Law, contact the copyright holder or the author.
dc.rightsAttribution 4.0 International (CC BY 4.0)*
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/*
dc.subject5′-norcarbocyclic nucleosidesen_US
dc.subjectmycobacterium tuberculosisen_US
dc.subjectantibacterial activityen_US
dc.subjecturacil derivativesen_US
dc.titleNovel 5′-Norcarbocyclic Pyrimidine Derivatives as Antibacterial Agentsen_US
dc.typeTexten_US

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