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Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 15; Vol. 29 (2), pp. 339-341. Date of Electronic Publication: 2018 Nov 09. - Publication Year :
- 2019
-
Abstract
- Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics.<br /> (Copyright © 2018. Published by Elsevier Ltd.)
- Subjects :
- Anti-HIV Agents chemical synthesis
Anti-HIV Agents chemistry
Dose-Response Relationship, Drug
Framycetin chemical synthesis
Framycetin chemistry
Molecular Structure
Neomycin analogs & derivatives
Neomycin chemistry
Structure-Activity Relationship
Anti-HIV Agents pharmacology
Framycetin pharmacology
HIV-1 drug effects
Neomycin pharmacology
RNA, Viral drug effects
Response Elements drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30477891
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.11.004