Synthesis and biological evaluation of sialylmimetics as rotavirus inhibitors.
Rotaviruses cause severe gastroenteritis in infants and are estimated to be responsible for over 600 000 deaths annually, primarily in developing countries. The development of potential inhibitors of this virus is therefore of great interest, particularly since the safety and efficacy of rotaviral vaccines has recently been questioned. This study describes the synthesis of a variety of compounds that can be considered as mimetics of N-acetylneuraminic acid thioglycosides and the subsequent in vitro biological evaluation of these sialylmimetics as inhibitors of rotaviral infection. Our results show that readily accessible carbohydrate-based compounds have the potential to act as inhibitors of rotaviral replication in vitro, presumably through inhibition of the rotaviral adhesion process.
Fazli
A
A
Centre for Biomolecular Science and Drug Discovery, Griffith University (Gold Coast Campus), PMB 50 Gold Coast Mail Centre, Queensland 9726, Australia.
Bradley
S J
SJ
Kiefel
M J
MJ
Jolly
C
C
Holmes
I H
IH
von Itzstein
M
M
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D002460:Cell Line; D006027:Glycosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D018716:Molecular Mimicry; D019158:N-Acetylneuraminic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009500:Neutralization Tests; D012401:Rotavirus / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D006027:Glycosides; D019158:N-Acetylneuraminic Acid