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SHR Neuro Krebs Kardio Lipid Stoffw Microb

de Castro, S; Fernández-Cureses, G; Andrei, G; Snoeck, R; Sánchez-Murcia, PA; Korba, B; Gago, F; Balzarini, J; Camarasa, MJ.
Conservation of antiviral activity and improved selectivity in PMEO-DAPym upon pyrimidine to triazine scaffold hopping.
Antiviral Res. 2015; 122(1):64-68 Doi: 10.1016/j.antiviral.2015.08.006
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Co-Autor*innen der Med Uni Graz
Sánchez Murcia Pedro Alejandro
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Abstract:
Acyclic nucleoside phosphonates incorporating 2,4-diaminotriazine (DAT) as a 5-aza-analog of the 2,4-diamino-pyrimidine (DAPym) nucleobase present in PMEO-DAPyms have been synthesized. The lead PMEO-DAT is as inhibitory against HIV, HBV, MSV and VZV replication as the parent PMEO-DAPym and equally inefficient at markedly affecting replication of HSV-1, HSV-2 and HCMV. A rationale for this similar biological profile is proposed on the basis of structural differences in the active site of the viral DNA polymerases. PMEO-DAT is, however, more selective because, unlike PMEO-DAPym, it does not stimulate secretion of β-chemokines in cultured PBMC. Copyright © 2015 Elsevier B.V. All rights reserved.
Find related publications in this database (using NLM MeSH Indexing)
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - pharmacology
Antiviral Agents - chemical synthesis
Antiviral Agents - pharmacology
Cells, Cultured -
Chemokines, CC - immunology
Chemokines, CC - metabolism
HIV-1 - drug effects
Herpesviridae - drug effects
Herpesvirus 1, Human - drug effects
Herpesvirus 2, Human - drug effects
Humans -
Leukocytes, Mononuclear - immunology
Models, Molecular -
Nucleosides -
Organophosphonates - chemistry
Organophosphonates - pharmacology
Pyrimidines - chemistry
Pyrimidines - pharmacology
Sarcoma Viruses, Murine - drug effects
Triazines - chemistry
Viruses - drug effects

Find related publications in this database (Keywords)
Polymerase inhibitors
Antivirals
Triazine
Phosphonates
Scaffold hopping
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