Cysteine-Targeted Insecticides against A. gambiae Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F20%3A00555732" target="_blank" >RIV/60162694:G44__/20:00555732 - isvavai.cz</a>
Alternative codes found
RIV/62690094:18470/20:50016707 RIV/00179906:_____/20:10410733
Result on the web
<a href="https://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.9b00477" target="_blank" >https://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.9b00477</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acsmedchemlett.9b00477" target="_blank" >10.1021/acsmedchemlett.9b00477</a>
Alternative languages
Result language
angličtina
Original language name
Cysteine-Targeted Insecticides against A. gambiae Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors
Original language description
Acetylcholinesterase cysteine-targeted insecticides against malaria vector Anopheles gambia 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 Anopheles gambiae 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 maleimide compounds.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry
Result continuities
Project
<a href="/en/project/NV16-34390A" target="_blank" >NV16-34390A: Development of new environment friendly insecticides against malaria mosquito</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
ACS Medicinal Chemistry Letters
ISSN
1948-5875
e-ISSN
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Volume of the periodical
11
Issue of the periodical within the volume
1
Country of publishing house
US - UNITED STATES
Number of pages
7
Pages from-to
65-71
UT code for WoS article
000526400900010
EID of the result in the Scopus database
2-s2.0-85076253292