Polysubstituted 4,6-bis(hetero)arylpyrimidines as dual inhibitors of nitric oxide and prostaglandin E-2 production
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00476117" target="_blank" >RIV/61388963:_____/17:00476117 - isvavai.cz</a>
Alternative codes found
RIV/68378041:_____/17:00476117
Result on the web
<a href="http://dx.doi.org/10.1016/j.niox.2017.05.001" target="_blank" >http://dx.doi.org/10.1016/j.niox.2017.05.001</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.niox.2017.05.001" target="_blank" >10.1016/j.niox.2017.05.001</a>
Alternative languages
Result language
angličtina
Original language name
Polysubstituted 4,6-bis(hetero)arylpyrimidines as dual inhibitors of nitric oxide and prostaglandin E-2 production
Original language description
As a part of our extensive structure -activity relationship study of anti-inflammatory heterocycles, a novel series of 67 polysubstituted 2-aminopyrimidines was prepared bearing one (at the C-4 position of the pyrimidine ring) or two (in the C-4 and C-6 positions) (hetero)aryl substituents attached directly through the C-C bond. The key synthetic steps involved either Suzuki-Miyaura or Stille cross-coupling reactions carried out on easily available 4,6-dichloropyrimidines. All prepared compounds, except one, were able to inhibit immune-activated production of nitric oxide (NO) significantly. Moreover, several compounds were found to be low micromolar dual inhibitors of NO and prostaglandin E-2 (PGE(2)) production. Although the exact mode of action of the prepared compounds remains to be elucidated, non-toxic dual inhibitors of NO and PGE2 production may have great therapeutic benefit in treatment of various inflammation diseases and deserve further preclinical evaluation.
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
10608 - Biochemistry and molecular biology
Result continuities
Project
<a href="/en/project/TE01020028" target="_blank" >TE01020028: Center for Development of Original Drugs</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Nitric Oxide-Biology and Chemistry
ISSN
1089-8603
e-ISSN
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Volume of the periodical
67
Issue of the periodical within the volume
Jul 1
Country of publishing house
NL - THE KINGDOM OF THE NETHERLANDS
Number of pages
5
Pages from-to
53-57
UT code for WoS article
000402849600006
EID of the result in the Scopus database
2-s2.0-85018785198