Design, synthesis and pharmacological evaluation of new anti-inflammatory compounds
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2016-08-30
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Resumo
Inflammatory diseases and pain are among the main problems that significantly influence the lifestyle of
millions of people and existing therapies are not always effective and can cause several adverse effects. In
this context, the molecular modifications or synthesis of compounds continue being the best strategies
for the identification of new compounds for the treatment of pain and inflammation. The aim of this
study was to evaluate the analgesic and anti-inflammatory activities of new analogues of pyrazole
compounds containing subunits N-phenyl-1-H-pirazoles and 1,3,4-oxadiazole-2(3H)-thione, LQFM-146,
LQFM-147 and LQFM-148. In the acetic acid-induced abdominal writhing test, treatments with LQFM146, LQFM-147 or LQFM-148 at doses 89, 178 and 356 mmol/kg p.o. reduced the abdominal writhing in a
dose-dependent manner. In the formalin test, these compounds at dose 178 mmol/kg p.o. reduced the
licking time only in inflammatory phase of this test, suggesting an antinociceptive effect dependent of
the anti-inflammatory effect. The treatment with the three compounds in intermediate dose (178 mmol/
kg p.o.) reduced the edema at all tested time points in the carrageenan-induced paw edema test and
reduced polymorphonuclears cell migration, activity myeloperoxidase and TNF-α levels in the carrageenan-induced pleurisy test. Our date suggest that the new compounds LQFM-146, LQFM-147 and
LQFM-148 possess satisfactory anti-inflammatory and antinociceptive effects that involves the reduction
of pro-inflammatory cytokines and inhibition of the myeloperoxidase enzyme.
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Pyrazole compounds, LQFM-146, LQFM-147, LQFM-148, Inflammation
Citação
CIDADE, Amanda F. et al. Design, synthesis and pharmacological evaluation of new anti-inflammatory compounds. European Journal of Pharmacology, Amsterdam, v. 791, p. 195-204, 2016. DOI: 10.1016/j.chemosphere.2016.08.144. Disponível em: https://www.sciencedirect.com/science/article/pii/S0014299916305520?via%3Dihub. Acesso em: 21 jun. 2023.