{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Gorecki L"],"funding":["Ministerstvo Zdravotnictví Ceské Republiky"],"pagination":["65-71"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6956356"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["11(1)"],"pubmed_abstract":["Acetylcholinesterase cysteine-targeted insecticides against malaria vector <i>Anopheles gambia</i> and other mosquitos have already been introduced. We have applied the olefin metathesis for the preparation of cysteine-targeted insecticides in high yields. The prepared compounds with either a succinimide or maleimide moiety were evaluated on <i>Anopheles gambiae</i> and human acetylcholinesterase with relatively high irreversible inhibition of both enzymes but poor selectivity. The concept of cysteine binding was not proved by several methods, and poor stability was observed of the chosen most potent/selective compounds in a water/buffer environment. Thus, our findings do not support the proposed concept of cysteine-targeted selective insecticides for the prepared series of succinimide or "],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Cysteine-Targeted Insecticides against <i>A. gambiae</i> Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors."],"pmcid":["PMC6956356"],"funding_grant_id":["NV16-34390A"],"pubmed_authors":["Hrabcova V","Bzonek P","Psotka M","Korabecny J","Musilek K","Kuca K","Kucera T","Jun D","Gorecki L","Hepnarova V","Schmidt M","Andrys R","Svobodova B"],"additional_accession":[]},"is_claimable":false,"name":"Cysteine-Targeted Insecticides against <i>A. gambiae</i> Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors.","description":"Acetylcholinesterase cysteine-targeted insecticides against malaria vector <i>Anopheles gambia</i> and other mosquitos have already been introduced. We have applied the olefin metathesis for the preparation of cysteine-targeted insecticides in high yields. The prepared compounds with either a succinimide or maleimide moiety were evaluated on <i>Anopheles gambiae</i> and human acetylcholinesterase with relatively high irreversible inhibition of both enzymes but poor selectivity. The concept of cysteine binding was not proved by several methods, and poor stability was observed of the chosen most potent/selective compounds in a water/buffer environment. Thus, our findings do not support the proposed concept of cysteine-targeted selective insecticides for the prepared series of succinimide or ","dates":{"release":"2020-01-01T00:00:00Z","publication":"2020 Jan","modification":"2026-05-04T19:45:11.068Z","creation":"2025-04-04T10:46:40.967Z"},"accession":"S-EPMC6956356","cross_references":{"pubmed":["31938465"],"doi":["10.1021/acsmedchemlett.9b00477"]}}