๐ Design, synthesis and evaluation of a series of acyclic fleximer nucleoside analogues with anti-coronavirus activity
ยฉ 2015 Elsevier Ltd. A series of doubly flexible nucleoside analogues were designed based on the acyclic sugar scaffold of acyclovir and the flex-base moiety found in the fleximers. The target compounds were evaluated for their antiviral potential and found to inhibit several coronaviruses. Significantly, compound 2 displayed selective antiviral activity (CC50 >3ร EC50) towards human coronavirus (HCoV)-NL63 and Middle East respiratory syndrome-coronavirus, but not severe acute respiratory syndrome-coronavirus. In the case of HCoV-NL63 the activity was highly promising with an EC50 <10 ฮผM and a CC50 >100 ฮผM. As such, these doubly flexible nucleoside analogues are viewed as a novel new class of drug candidates with potential for potent inhibition of coronaviruses.
keywords
๐ severe acute (1373)
๐ human coronavirus (623)
๐ respiratory syndrome (2004)
๐ acute respiratory (1734)
author
๐ค Peters, Hannah L.
๐ค Jochmans, Dirk
๐ค De Wilde, Adriaan H.
๐ค Posthuma, Clara C.
๐ค Snijder, Eric J.
๐ค Neyts, Johan
๐ค Seley-Radtke, Katherine L.
year
โฐ 2015
issn
๐ 14643405 0960894X
volume
25
number
15
page
2923-2926
citedbycount
19
download
๐ [BibTeX]