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 coun tries. The development of potential inhibitors of this virus is therefore o f great interest, particularly since the safety and efficacy of rotaviral v accines has recently been questioned. This study describes the synthesis of a variety of compounds that can be considered as mimetics of N-acetylneura minic 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 potentia l to act as inhibitors of rotaviral replication in vitro, presumably throug h inhibition of the rotaviral adhesion process.