Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase

scientific article

Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1016/J.BMCL.2015.09.019
P932PMC publication ID4593063
P698PubMed publication ID26386602

P50authorPaul R. CarlierQ40443285
Aaron GrossQ47698089
Dawn M WongQ58865571
P2093author name stringJianyong Li
Jeffrey R Bloomquist
Rafique Islam
Elisabet Viayna
James M Mutunga
Fan Tong
Maxim M Totrov
Eugene Camerino
Florian Körber
P2860cites workA new and rapid colorimetric determination of acetylcholinesterase activityQ26778487
A structure-based design approach to the development of novel, reversible AChE inhibitorsQ27634903
Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmineQ27638306
Synopsis of some recent tactical application of bioisosteres in drug designQ34171394
Select small core structure carbamates exhibit high contact toxicity to "carbamate-resistant" strain malaria mosquitoes, Anopheles gambiae (Akron).Q34437731
3-Oxoisoxazole-2(3H)-carboxamides and isoxazol-3-yl carbamates: Resistance-breaking acetylcholinesterase inhibitors targeting the malaria mosquito, Anopheles gambiaeQ35137440
Re-engineering aryl methylcarbamates to confer high selectivity for inhibition of Anopheles gambiae versus human acetylcholinesteraseQ36074233
Docking and scoring with ICM: the benchmarking results and strategies for improvementQ36098710
Aryl methylcarbamates: potency and selectivity towards wild-type and carbamate-insensitive (G119S) Anopheles gambiae acetylcholinesterase, and toxicity to G3 strain An. gambiaeQ36625717
Malaria vector control at a crossroads: public health entomology and the drive to eliminationQ38227819
Control of pyrethroid-resistant Anopheles gambiae and Culex quinquefasciatus mosquitoes with chlorfenapyr in BeninQ39288227
Fluorinated aldehydes and ketones acting as quasi-substrate inhibitors of acetylcholinesteraseQ41607860
Fluoro ketone inhibitors of hydrolytic enzymesQ42205010
Toxicities of 31 volatile low molecular weight compounds against Aedes aegypti and Culex quinquefasciatusQ42986765
Vapor toxicity of three prototype volatile insecticidal compounds to house fly (Diptera: Muscidae).Q43229998
Structure-activity studies of fluoroketone inhibitors of alpha-lytic protease and human leukocyte elastaseQ43479298
Comparative genomics: Insecticide resistance in mosquito vectorsQ44150921
A new amino-acid substitution in acetylcholinesterase 1 confers insecticide resistance to Culex pipiens mosquitoes from Cyprus.Q44170998
Insecticide resistance in disease vectors of public health importanceQ44172412
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acidQ44774451
Heterocyclic derivatives of 3-substituted-1,1,1-trifluoro-2-propanones as inhibitors of esterolytic enzymes.Q45951016
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acidsQ46986323
Flexible protein-ligand docking by global energy optimization in internal coordinates.Q52281044
Inhibition of serine proteases by peptidyl fluoromethyl ketonesQ68893782
Molecular recognition in acetylcholinesterase catalysis: free-energy correlations for substrate turnover and inhibition by trifluoro ketone transition-state analogsQ72061964
Effect of MDL 73,745 on acetylcholine and biogenic amine levels in rat cortexQ72314280
Substrate and product trafficking through the active center gorge of acetylcholinesterase analyzed by crystallography and equilibrium bindingQ79892396
P433issue20
P407language of work or nameEnglishQ1860
P921main subjectAnopheles gambiaeQ135237
P304page(s)4405-4411
P577publication date2015-09-08
P1433published inBioorganic & Medicinal Chemistry LettersQ2709483
P1476titleDifluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase
P478volume25

Reverse relations

cites work (P2860)
Q48334564CF2H, a Hydrogen Bond Donor.
Q39125732Discovery of Species-selective and Resistance-breaking Anticholinesterase Insecticides for the Malaria Mosquito
Q90322929Select β- and γ-branched 1-alkylpyrazol-4-yl methylcarbamates exhibit high selectivity for inhibition of Anopheles gambiae versus human acetylcholinesterase
Q48020171Structure of the G119S Mutant Acetylcholinesterase of the Malaria Vector Anopheles gambiae Reveals Basis of Insecticide Resistance

Search more.