PubMed:35849863 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PubMed/sourceid/35849863","sourcedb":"PubMed","sourceid":"35849863","source_url":"https://www.ncbi.nlm.nih.gov/pubmed/35849863","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.","tracks":[{"project":"HP-phenotype","denotations":[{"id":"T1","span":{"begin":224,"end":228},"obj":"Phenotype"}],"attributes":[{"id":"A1","pred":"hp_id","subj":"T1","obj":"HP:6000789"},{"subj":"T1","pred":"source","obj":"HP-phenotype"}],"namespaces":[{"prefix":"HP","uri":"http://purl.obolibrary.org/obo/HP_"}]},{"project":"NCBITAXON","denotations":[{"id":"T1","span":{"begin":224,"end":228},"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":"381124"},{"id":"A2","pred":"db_id","subj":"T2","obj":"93504"},{"id":"A3","pred":"db_id","subj":"T3","obj":"51655"},{"subj":"T1","pred":"source","obj":"NCBITAXON"},{"subj":"T2","pred":"source","obj":"NCBITAXON"},{"subj":"T3","pred":"source","obj":"NCBITAXON"}]}],"config":{"attribute types":[{"pred":"source","value type":"selection","values":[{"id":"HP-phenotype","color":"#ec93c7","default":true},{"id":"NCBITAXON","color":"#93e1ec"}]}]}}