Ontology highlight
ABSTRACT:
SUBMITTER: Hartsel JA
PROVIDER: S-EPMC3389130 | biostudies-literature | 2012 Jul
REPOSITORIES: biostudies-literature
Hartsel Joshua A JA Wong Dawn M DM Mutunga James M JM Ma Ming M Anderson Troy D TD Wysinski Ania A Islam Rafique R Wong Eric A EA Paulson Sally L SL Li Jianyong J Lam Polo C H PC Totrov Maxim M MM Bloomquist Jeffrey R JR Carlier Paul R PR
Bioorganic & medicinal chemistry letters 20120606 14
To identify potential human-safe insecticides against the malaria mosquito we undertook an investigation of the structure-activity relationship of aryl methylcarbamates inhibitors of acetylcholinesterase (AChE). Compounds bearing a β-branched 2-alkoxy or 2-thioalkyl group were found to possess good selectivity for inhibition of Anopheles gambiae AChE over human AChE; up to 530-fold selectivity was achieved with carbamate 11d. A 3D QSAR model is presented that is reasonably consistent with log in ...[more]