Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues. Issue 2 (15th January 2019)

• Record Type: Journal Article
• Authors: Simon, Binto; Walmsley, Claire; Jackson, Victoria J.; Garvey, Edward P.; Slater, Martin J.; Berrisford, David J.; Gardiner, John M.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 2(2019)
• Page Start: 339
• Page End: 341
• Publication Date: 2019-01-15
• Subjects: Neomycin -- Neamine -- RNA RRE -- HIV-1 -- Aminoglycosides; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.11.004
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.