Full metadata record
DC Field | Value | Language |
---|---|---|
dc.creator | Santivañez-Veliz, M. (Mery) | - |
dc.creator | Pérez-Silanes, S. (Silvia) | - |
dc.creator | Torres, E. (Enrique) | - |
dc.creator | Moreno-de-Viguri, E. (Elsa) | - |
dc.date.accessioned | 2016-04-25T16:35:42Z | - |
dc.date.available | 2016-04-25T16:35:42Z | - |
dc.date.issued | 2016 | - |
dc.identifier.citation | Santivañez-Veliz M, Pérez-Silanes S, Torres E, Moreno-Viguri E. Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis. Bioorg Med Chem Lett 2016;26(9):2188–2193 | es_ES |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://hdl.handle.net/10171/40412 | - |
dc.description.abstract | Abstract Twenty-four quinoxaline derivatives were evaluated for their antimycobacterial activity using BacTiter-Glo microbial cell viability assay. Five compounds showed MIC values < 3.1 μM and IC50 values < 1.5 μM in primary screening and therefore, they were moved on for further evaluation. Compounds 21 and 18 stand out, showing MIC values of 1.6 μM and IC50 values of 0.5 and 1.0 μM respectively. Both compounds were the most potent against three evaluated drug-resistant strains. Moreover, they exhibited intracellular activity in infected macrophages, considering log-reduction and cellular viability. In addition, compounds 16 and 21 were potent against non-replicating M. Tb. and compound 21 was bactericidal. Therefore, quinoxaline derivatives could be considered for making further advances in the future development of antimycobacterial agents. | es_ES |
dc.description.sponsorship | Federal funds from the Division of Microbiology and Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Department of Health and Human Services, under Contract No. HHSN272201100009I”.Government of Navarra for grant “International Talent” and with University of Navarra for a grant. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | Elsevier | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | * |
dc.subject | Tuberculosis | es_ES |
dc.subject | Antimycobacterial | es_ES |
dc.subject | Quinoxaline | es_ES |
dc.subject | Intracellular activity | es_ES |
dc.title | Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.identifier.doi | http://dx.doi.org/10.1016/j.bmcl.2016.03.066 | es_ES |
Files in This Item:
Statistics and impact
Items in Dadun are protected by copyright, with all rights reserved, unless otherwise indicated.