Anti-inflammatory, ulcerogenic and platelet activation evaluation of novel 1,4-diaryl-1,2,3-triazole neolignan-celecoxib hybrids

Felipe, Josyelen Lousada; Cassamale, Tatiana B.; Lourenço, Leticia D.; Carvalho, Diego B.; Neves, Amarith R. das; Duarte, Rita Carolina Figueiredo; Carvalho, Maria G.; Toffoli-Kadri, Mônica Cristina; Baroni, Adriano C. M.

doi:10.1016/j.bioorg.2021.105485

Cited by 17 publications

(6 citation statements)

References 60 publications

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“…This event might be related to a possible level of the anti-inflammatory effect exerted by the isoxazole analogues. Literature showed the anti-inflammatory potential of neolignan-based compounds bearing a triazole core, a bioisostere of the isoxazole core that also presents anti-inflammatory activity . Further research might explore the anti-inflammatory potential of isoxazole analogues described in this work.…”

Section: Resultsmentioning

confidence: 99%

In Vivo Antileishmanial Effect of 3,5-Diaryl-isoxazole Analogues Based on Veraguensin, Grandisin, and Machilin G: A Glance at a Preclinical Study

et al. 2023

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New treatment approaches targeting cutaneous leishmaniasis (CL) are required since conventional drugs exhibit limitations due to their several adverse effects and toxicity. In this study, we aimed to evaluate the in vivo intralesional treatment efficacy of five isoxazole derivatives previously synthesized and effective in vitro against intracellular amastigote forms of Leishmania (L.) amazonensis. Among the tested analogues, 7 exhibited relevant in vivo therapeutic effects. The in silico predictions provided interesting information about the toxicity, suggesting the safety of analogue 7. Experiments performed with Salmonella typhimurium strains (TA98, TA100, and TA102) showed a non-mutagenicity profile of 7. The treatment of Leishmania-infected BALB/c mice with isoxazole 7 showed remarkably smaller CL lesions and decreased the parasitism (by 98.4%) compared to the control group. Hence, analogue 7 is a promising drug candidate and alternative treatment for CL caused by L. amazonensis.

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Section: Resultsmentioning

confidence: 99%

In Vivo Antileishmanial Effect of 3,5-Diaryl-isoxazole Analogues Based on Veraguensin, Grandisin, and Machilin G: A Glance at a Preclinical Study

et al. 2023

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“…Targeting COX-2, NF-kB, STAT3, and histone acetylation involved in the inflammatory process could represent a good strategy for anti-inflammatory activity, cancer prevention, and therapy. [151][152][153][154][155][156][157]…”

Section: Miscellaneous Heterocycles As Anti-inflammatory Agentsmentioning

confidence: 99%

Small Molecules as Anti‐inflammatory Agents: Molecular Mechanisms and Heterocycles as Inhibitors of Signaling Pathways

Basha¹

2023

ChemistrySelect

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Cancer and inflammation interlink with many pathways. Millions of people died because of these two disorders. Major pathways that cause both inflammation and cancer are STAT3, NF‐κB, COX, and histone acetylation. However, these are the target for medicinally potent heterocycles such as pyrimidines, indole, and pyrazole. Many NSAIDs reported in the literature belong to both natural and synthetic molecules. This review encompasses molecular mechanisms for inflammation, NSAIDs derived from natural sources and synthetic methods, and recent reports on heterocycles as potent anti‐inflammatory agents and their significance in cancer treatment. Literature for the study, accomplished from 2019 to 2022.

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“…Among the evaluated compounds, 2 showed the most significant activity with an IC 50 value of 18 μM against the KKU-213 cell line, which was eight-fold more effective than acanthoic acid. An assessment of anti-inflammatory, ulcerogenic, platelet activation activities, and the molecular docking studies of COX-2 and P-selectin of the 1,4-diaryl-1,2,3-triazole hybrids has been recently published [ 18 ]. The analogs 3 – 5 exhibited anti-inflammatory activity and lacked the induction of gastric lesions in mice when compared to the reference drug, indomethacin.…”

Section: Five-membered Heterocyclic Compoundsmentioning

confidence: 99%

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

Ebenezer

Jordaan

Carena

et al. 2022

IJMS

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Heterocyclic compounds are a class of compounds of natural origin with favorable properties and hence have major pharmaceutical significance. They have an exceptional adroitness favoring their use as diverse smart biomimetics, in addition to possessing an active pharmacophore in a complex structure. This has made them an indispensable motif in the drug discovery field. Heterocyclic compounds are usually classified according to the ring size, type, and the number of heteroatoms present in the ring. Among different heterocyclic ring systems, nitrogen heterocyclic compounds are more abundant in nature. They also have considerable pharmacological significance. This review highlights recent pioneering studies in the biological assessment of nitrogen-containing compounds, namely: triazoles, tetrazoles, imidazole/benzimidazoles, pyrimidines, and quinolines. It explores publications between April 2020 and February 2022 and will benefit researchers in medicinal chemistry and pharmacology. The present work is organized based on the size of the heterocyclic ring.

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Anti-inflammatory, ulcerogenic and platelet activation evaluation of novel 1,4-diaryl-1,2,3-triazole neolignan-celecoxib hybrids

Cited by 17 publications

References 60 publications

In Vivo Antileishmanial Effect of 3,5-Diaryl-isoxazole Analogues Based on Veraguensin, Grandisin, and Machilin G: A Glance at a Preclinical Study

In Vivo Antileishmanial Effect of 3,5-Diaryl-isoxazole Analogues Based on Veraguensin, Grandisin, and Machilin G: A Glance at a Preclinical Study

Small Molecules as Anti‐inflammatory Agents: Molecular Mechanisms and Heterocycles as Inhibitors of Signaling Pathways

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds

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