PubMed:35849863 JSONTXT

{"project":"GlyCosmos6-CLO","denotations":[{"id":"T1","span":{"begin":409,"end":417},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"},{"id":"T2","span":{"begin":646,"end":654},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"},{"id":"T3","span":{"begin":737,"end":745},"obj":"http://purl.obolibrary.org/obo/CLO_0001658"}],"text":"Design, synthesis, biologically evaluation and molecular docking of C-glycosidic oximino carbamates as novel OfHex1 inhibitors.\nThe inhibition of function-specific β-N-acetyl-D-hexosaminidases, such as OfHex1 from the Asian corn borer (Ostrinia furnacalis), is a promising strategy for the development of green pesticides. Among reported OfHex1 inhibitors, glycosyl inhibitors show especially high inhibitory activity. In this study, a series of novel C-glycosidic oximino carbamate derivatives were designed using the OfHex1 crystal structure and synthesized. Among the C-Glycoside derivatives studied, compound 7k exhibited the best inhibitory activity against OfHex1 (IC50 = 47.47 μM). Compound 7k also exhibited excellent larvicidal activity against Plutella xylostella. The potential inhibitory mechanism of 7k was studied using molecular docking. Notably, compound 7k is the first reported C-glycoside inhibitor of OfHex1. These results provide direction for the rational design of novel OfHex1 inhibitors."}

{"project":"NCBITAXON","denotations":[{"id":"T1","span":{"begin":218,"end":234},"obj":"OrganismTaxon"},{"id":"T2","span":{"begin":236,"end":255},"obj":"OrganismTaxon"},{"id":"T3","span":{"begin":754,"end":773},"obj":"OrganismTaxon"}],"attributes":[{"id":"A1","pred":"db_id","subj":"T1","obj":"NCBItxid:93504"},{"id":"A2","pred":"db_id","subj":"T2","obj":"NCBItxid:93504"},{"id":"A3","pred":"db_id","subj":"T3","obj":"NCBItxid:51655"}],"text":"Design, synthesis, biologically evaluation and molecular docking of C-glycosidic oximino carbamates as novel OfHex1 inhibitors.\nThe inhibition of function-specific β-N-acetyl-D-hexosaminidases, such as OfHex1 from the Asian corn borer (Ostrinia furnacalis), is a promising strategy for the development of green pesticides. Among reported OfHex1 inhibitors, glycosyl inhibitors show especially high inhibitory activity. In this study, a series of novel C-glycosidic oximino carbamate derivatives were designed using the OfHex1 crystal structure and synthesized. Among the C-Glycoside derivatives studied, compound 7k exhibited the best inhibitory activity against OfHex1 (IC50 = 47.47 μM). Compound 7k also exhibited excellent larvicidal activity against Plutella xylostella. The potential inhibitory mechanism of 7k was studied using molecular docking. Notably, compound 7k is the first reported C-glycoside inhibitor of OfHex1. These results provide direction for the rational design of novel OfHex1 inhibitors."}