This study presents the first class of oxadiazole-based macrocyclic inhibitors targeting norovirus 3CL protease, offering a potential therapeutic avenue for norovirus infections.
Cell-permeable oxadiazole macrocycles inhibit norovirus 3CL protease in vitro; leaves open therapeutic translation pending in vivo studies.
Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.
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Damalanka et al. (2016) studied this question.
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