Anti-inflammatory activity of novel thiosemicarbazone compounds indole-based as COX inhibitors

Jacob, Iris Trindade Tenório; Gomes, Filipa; Miranda, Mirelly Dianne Santos de; Almeida, Sinara Mônica Vitalino de; Filho, Iranildo José da Cruz; Peixoto, Christina Alves; Silva, Teresinha G. da; Moreira, Diogo Rodrigo Magalhães; Melo, Cristiane Moutinho Lagos de; Oliveira, Jamerson Ferreira de; Lima, Maria Alice Gomes de Andrade

doi:10.1007/s43440-021-00221-7

Cited by 39 publications

(32 citation statements)

References 68 publications

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“…It is an indicator of safety and efficacy of compounds with pharmacological potential. The higher this index, the greater the potential use of these compounds in future clinical tests, with an SI above 3 being promising [ 49 ].…”

Section: Resultsmentioning

confidence: 99%

Evaluation of Toxicity and Oxidative Stress of 2-Acetylpyridine-N(4)-orthochlorophenyl Thiosemicarbazone

Lira

Parrilha

Dias

et al. 2022

Oxidative Medicine and Cellular Longevity

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Thiosemicarbazones are well known for their broad spectrum of action, including antitumoral and antiparasitic activities. Thiosemicarbazones work as chelating binders, reacting with metal ions. The objective of this work was to investigate the in silico, in vitro, and in vivo toxicity and oxidative stress of 2-acetylpyridine-N(4)-orthochlorophenyl thiosemicarbazone (TSC01). The in silico prediction showed good absorption by biological membranes and no theoretical toxicity. Also, the compound did not show cytotoxicity against Hep-G2 and HT-29 cells. In the acute nonclinical toxicological test, the animals treated with TSC01 showed behavioral changes of stimulus of the central nervous system (CNS) at 300 mg/kg. One hour after administration, a dose of 2000 mg/kg caused depressive signs. All changes disappeared after 24 h, with no deaths, which suggest an estimated LD50 of 5000 mg/kg and GSH 5. The group treated with 2000 mg/kg had an increase of water consumption and weight gain in the second week. The biochemical parameters presented no toxicity relevance, and the analysis of oxidative stress in the liver found an increase of lipid peroxidation and nitric oxide. However, histopathological analysis showed organ integrity was maintained without any changes. In conclusion, the results show the low toxicological potential of thiosemicarbazone derivative, indicating future safe use.

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Section: Resultsmentioning

confidence: 99%

Evaluation of Toxicity and Oxidative Stress of 2-Acetylpyridine-N(4)-orthochlorophenyl Thiosemicarbazone

Lira

Parrilha

Dias

et al. 2022

Oxidative Medicine and Cellular Longevity

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“…This compound was able to inhibit lymphocyte proliferation, with IC 50 = 0.5 ± 0.07 μM and displayed better results than indomethacin (IC 50 > 12 μM) and was also found to suppress the in vitro production of TNF-α and NO, in addition to stimulating the production of IL-4. 87 Chen et al thesis began via C-3 alkylation of 5-methoxy indole 201 followed by bromination and hydrolysis to afford 204. The compound 207 was prepared using esterification of compound 205 followed by protection of the amine group of compound 206.…”

Section: Reported Indoles As Antiinflammatory Agentsmentioning

confidence: 99%

The indole nucleus as a selective COX-2 inhibitor and anti-inflammatory agent (2011–2022)

et al. 2022

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“…The phenoxy acetamide, indole, chalcone thiosemicarbazone, and quinoline are important groups in anti-inflammatory agents [ 47 , 107 , 108 ]. Huang, Qian, and coworkers designed indole-2-amides as anti-inflammatory drugs [ 33 , 109 ].…”

Section: Multitarget Drugsmentioning

confidence: 99%

The Role of Organic Small Molecules in Pain Management

Cuesta

Meneses

2021

Molecules

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In this review, a timeline starting at the willow bark and ending in the latest discoveries of analgesic and anti-inflammatory drugs will be discussed. Furthermore, the chemical features of the different small organic molecules that have been used in pain management will be studied. Then, the mechanism of different types of pain will be assessed, including neuropathic pain, inflammatory pain, and the relationship found between oxidative stress and pain. This will include obtaining insights into the cyclooxygenase action mechanism of nonsteroidal anti-inflammatory drugs (NSAID) such as ibuprofen and etoricoxib and the structural difference between the two cyclooxygenase isoforms leading to a selective inhibition, the action mechanism of pregabalin and its use in chronic neuropathic pain, new theories and studies on the analgesic action mechanism of paracetamol and how changes in its structure can lead to better characteristics of this drug, and cannabinoid action mechanism in managing pain through a cannabinoid receptor mechanism. Finally, an overview of the different approaches science is taking to develop more efficient molecules for pain treatment will be presented.

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Anti-inflammatory activity of novel thiosemicarbazone compounds indole-based as COX inhibitors

Cited by 39 publications

References 68 publications

Evaluation of Toxicity and Oxidative Stress of 2-Acetylpyridine-N(4)-orthochlorophenyl Thiosemicarbazone

Evaluation of Toxicity and Oxidative Stress of 2-Acetylpyridine-N(4)-orthochlorophenyl Thiosemicarbazone

The indole nucleus as a selective COX-2 inhibitor and anti-inflammatory agent (2011–2022)

The Role of Organic Small Molecules in Pain Management

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