Antipyretic and antioxidant activities of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles in rats

Pasin, Juliana Saibt Martins; Ferreira, Ana Paula Oliveira; Saraiva, André Lopes; Ratzlaff, Viviane; Andrighetto, Rosália; Machado, Pablo; Marchesan, Sara; Zanette, Régis A.; Bonacorso, Hélio G.; Zanatta, Nilo; Martins, Marcos A. P.; Ferreira, João Paulo Gonçalves; Mello, Carlos Fernando

doi:10.1590/s0100-879x2010007500139

Cited by 31 publications

(12 citation statements)

References 33 publications

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“…Well‐known samples are Celecoxib (Celebrex) and Sildenafil (Viagra). Products of pyrazoles have been exposed to possess diverse properties including, but not restricted to, being antitumor, antidiabitic, anti‐inflammatory, antiarrhythmic, monoamine oxidase inhibiting, sPLA2‐inhibitory, antipyretic, analgesic, anticonvulsant, and antimicrobial . In fact, preparation method equally represents a pivotal role to discover the biologically active pyrazoles and their belongings.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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The major diseases spread in the environment only because of microbes. Even, intensive care units in the hospitals are polluted by microorganisms, particularly, Gram-positive bacteria. Although many antibiotics are existed, there is a need to develop up to date microbial-resistant agents. Hence, the current study aimed to develop prominent antimicrobial drug-related compounds. Thus, a novel series of tri-substituted analogs and their intermediates were synthesized. In addition, total new compounds were screened for their antimicrobial assay and identified as the most efficient biologically active compounds. Moreover, minimal inhibitory antimicrobial activity and appropriate structure activity relationships were investigated. From the results it was observed that, viability of Gram-positive bacteria was most powerfully affected by all active compounds. Finally, this research demonstrated that, these biologically energetic amalgams can be utilized for further preclinical studies with the ambition of standing unique inventive drugs.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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“…However, they often produce significant side effects and are toxic to various organs of the body, causing problems such as kidney failure, allergic reactions, reduced auditory ability, and increased risk of hemorrhage due to interference with platelet function [1,2]. erefore, the development of novel compounds with analgesic and antipyretic activities without side effects are needed [3].…”

Section: Introductionmentioning

confidence: 99%

Analgesic and Antipyretic Activities of Ethyl Acetate Fraction Tablet of Andrographis paniculata in Animal Models

Ilmi

Pamungkas

Tumewu

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Objectives. To determine the analgesic and antipyretic activities of a tablet derived from Andrographis paniculata ethyl acetate fraction (AS201-01) in animal models. Methods. The tablet derived from AS201-01 contains an equivalent of 35 mg andrographolide per tablet. Analgesic activity was determined using an acetic acid-induced writhing test on adult male mice. A writhe was recorded by a stopwatch and was defined as the stretching of the abdomen and/or stretching of at least one hind limb. For the determination of antipyretic activity, pyrexia was induced by subcutaneous injection of 15% w/v Brewer’s yeast into adult male rats. Rectal temperature was monitored at 1, 2, 3, and 4 hours after treatment. Results. The results showed that the AS201-01 tablet had analgesic and antipyretic activity. In the acetic acid-induced writhing model, AS201-01 tablet exhibited significant analgesic effect with a 66.73% reduction in writhing response at a dose of 50 mg andrographolide/kg body weight compared to the negative control group. The tablet also showed a significant antipyretic effect. The maximum antipyretic effect was observed after the third hour of administration of the AS201-01 tablet at a dose of 100 mg andrographolide/kg body weight. Conclusion. Tablet of Andrographis paniculata ethyl acetate fraction (AS201-01) exhibited analgesic and antipyretic activities.

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“…The pyrazole ring, bearing atoms of at least two different elements as a member of its ring, is considered to be a privileged structure and an attractive scaffold for drug discovery [10,11]. Pyrazole derivatives represent one of the most active classes of compounds and exhibit a broad spectrum of pharmacological activities, such as antimicrobial [12,13], analgesic [14,15], anti-inflammatory [16e18], antipyretic [15,19], cardiovascular [20] and anticancer [21,22] activities, among others effects.…”

Section: Introductionmentioning

confidence: 99%

Potential anti-inflammatory effect of LQFM-021 in carrageenan-induced inflammation: The role of nitric oxide

Florentino

Silva

et al. 2017

Nitric Oxide

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The pyrazole compound LQFM-021 exhibits vasorelaxant, antinociceptive and anti-inflammatory activities. Furthermore, it has low toxicity, indicating that this compound may be considered to be a good prototype for the development of new analgesic/anti-inflammatory drugs. Therefore, the aim of this study was to investigate the potential anti-inflammatory activity of LQFM-021 using a model of carrageenan-induced inflammation as well as the mechanism of action and role of nitric oxide in this effect. Acute treatments with LQFM-021 (30 and 60 mg/kg p.o.) reduced paw edema formation dose-dependently 2 h after carrageenan injection. In the carrageenan-induced pleurisy test, LQFM-021 (30 mg/kg p.o.) reduced the leukocyte (polymorphonuclear) count in the pleural cavity, as well as decreased protein extravasation and myeloperoxidase activity. This dose of LQFM-021 increased the NO (nitrite/nitrate) and IL-4 levels and decreased the TNF-α and IL-1β levels in the pleural cavity. Moreover, pre-treatment with L-NAME reversed the effect of LQFM-021 on NO, leukocyte migration, and the TNF-α and IL-1β levels. Additionally, we observed that LQFM-021 showed weak inhibitory activity on cyclooxygenases, but reduced the PGE levels in the pleural cavity. Immunoblot analyses showed that LQFM-021 promoted a decrease in COX-2 levels and increase in iNOS levels. In conclusion, we demonstrated that LQFM-021 has marked anti-inflammatory activity by reducing polymorphonuclear recruitment, which is associated with the inhibition of the production of inflammatory cytokines and eicosanoids. In addition, we found that the synthase/release of nitric oxide promoted by LQFM-021 is essential for the anti-inflammatory effect observed.

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Antipyretic and antioxidant activities of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles in rats

Cited by 31 publications

References 33 publications

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Analgesic and Antipyretic Activities of Ethyl Acetate Fraction Tablet of Andrographis paniculata in Animal Models

Potential anti-inflammatory effect of LQFM-021 in carrageenan-induced inflammation: The role of nitric oxide

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