New Substituted 5-Benzylideno-2-Adamantylthiazol[3,2-b][1,2,4]Triazol-6(5H)ones as Possible Anti-Inflammatory Agents

作者: Christophe Tratrat , Aliki Paparisva , Antonis Gavalas , Athina Geronikaki , Katharigatta N. Venugopala

DOI: 10.3390/MOLECULES26030659

关键词: PharmacologyCarrageenanNaproxenDocking (molecular)Anti-inflammatoryLipoxygenaseIn vivoChemistryCyclooxygenaseAutoDock

摘要: Background: Inflammation is a complex response to noxious stimuli promoted by the release of chemical mediators from damaged cells. Metabolic products arachidonic acid, produced action cyclooxygenase and lipoxygenase, play important roles in this process. Several non-steroidal anti-inflammatory drugs act as inhibitors. However, almost all them have undesired side effects. Methods: Prediction compounds was performed using PASS Program. The activity evaluated carrageenan paw edema test. COX LOX inhibitory actions were tested ovine COX-1, human recombinant COX-2 soybean LOX-1, respectively. Docking analysis Autodock. Results: All designed derivatives had good prediction results according synthesized experimentally evaluated. exhibited vivo with eleven being equal or better than indomethacin. Although, some no low effect on COX-1/2 LOX, certain COX-1 inhibition much higher naproxen inhibition, well explained analysis. Conclusions: A number obtained. remarkable did not follow results, indicating implication other mechanisms.

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