Identification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights

Badawi, Waleed A.; Rashed, Mahmoud; Nocentini, Alessio; Bonardi, Alessandro; Abd‐Αlhaseeb, Mohammad M.; Al-Rashood, Sara T.; Veerakanellore, Giri Babu; Majrashi, Taghreed A.; Elkaeed, Eslam B.; Elgendy, Bahaa; Gratteri, Paola; Supuran, Claudiu T.; Eldehna, Wagdy M.; Elagawany, Mohamed

doi:10.1080/14756366.2023.2201407

Cited by 4 publications

(1 citation statement)

References 59 publications

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“…Compound 82a was nonulcerogenic, while compound 82b showed some damage to the rat stomach. They noticed that the methanesulfonate and ethanesulfonate pyridazinone derivatives (82a and 82b) had the most effective and selective COX-2 inhibitory activity (Figure 12) (Badawi et al, 2023). showed comparable inhibitory activity to indomethacin (56.8%) with percentage of edema inhibition at 6 h of 49.7, and 53.6%, respectively.…”

Section: Cox-2 Inhibitory Activity Of 26disubstituted Pyridazine Deri...mentioning

confidence: 99%

Pyridazine derivatives as selective COX‐2 inhibitors: A review on recent updates

Ewieda,

Ahmed,

Hassan

et al. 2023

Drug Development Research

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Selective cyclooxygenase (COX)‐2 inhibitors have several advantages over nonselective COX inhibitors (nonsteroidal anti‐inflammatory drugs [NSAIDs]), including the absence of adverse effects (renal and hepatic disorders) associated with the long‐term use of standard NSAIDs, as well as an improved gastrointestinal profile. The pyridazine nucleus is regarded as a promising scaffold for the development of powerful COX‐2 inhibitors, particularly when selectively functionalized. This article summarizes some methods for the synthesis of pyridazine derivatives. Furthermore, it covers all of the pyridazine derivatives that have appeared as selective COX‐2 inhibitors, making it useful as a reference for the rational design of novel selective COX‐2 inhibitors.

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Section: Cox-2 Inhibitory Activity Of 26disubstituted Pyridazine Deri...mentioning

confidence: 99%

Pyridazine derivatives as selective COX‐2 inhibitors: A review on recent updates

Ewieda,

Ahmed,

Hassan

et al. 2023

Drug Development Research

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Synthesis, Spectroscopic Characterization, Antibacterial Activity, Reactivity Parameters, and Molecular Docking Studies of Some Pyridazine Derivatives

Daoui,

Parlak,

Direkel

et al. 2024

ChemistrySelect

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Three novel 4‐aryl‐2‐(2‐(4‐fluorophenyl)‐2‐oxoethyl)‐6‐phenylpyridazin‐3(2H)‐one derivatives were synthesized, and their chemical structures were established based on 1H‐NMR, 13C‐NMR, ESI‐HRMS, and FT‐IR spectral data. Their in vitro antibacterial activities were evaluated against Staphylococcus aureus [MRSA] (Gram‐positive isolate), Escherichia coli and Salmonella typhimurium (Gram‐negative isolates), and Pseudomonas aeruginosa and Acinetobacter baumannii (Gram‐negative nonfermenter isolates), and the results were compared with the standard drug “Amikacin”. The results showed that one of the compounds has good antibacterial activity against P. aeruginosa (MIC = 11.57 µM) and E. coli (MIC = 23.14 µM). In order to gain molecular insights into the compounds, their reactivity properties were studied using density functional theory (DFT), and molecular docking was carried out for the compounds with E. coli MurB protein receptors (2Q85).

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Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies

Begines,

Bonardi,

Nocentini

et al. 2023

Bioorganic & Medicinal Chemistry

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Identification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights

Cited by 4 publications

References 59 publications

Pyridazine derivatives as selective COX‐2 inhibitors: A review on recent updates

Pyridazine derivatives as selective COX‐2 inhibitors: A review on recent updates

Synthesis, Spectroscopic Characterization, Antibacterial Activity, Reactivity Parameters, and Molecular Docking Studies of Some Pyridazine Derivatives

Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies

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