Diarrea por Clostridium difficile

Paula, José María Prieto de; Ares, Enrique Guillem; Nicás, Vicente Villamandos; Fuente, Hortensia Sanz de la

doi:10.1016/s0025-7753(01)72097-0

Cited by 3 publications

(1 citation statement)

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“…are two commercially available indazole‐containing analgesic and anti‐inflammatory agents, but the first one was withdrawn from the market due to risks of hepatotoxicity (Figure 1). [ 23 ]…”

Section: Introductionmentioning

confidence: 99%

Anti‐inflammatory and analgesic effect of LD‐RT and some novel thiadiazole derivatives through COX‐2 inhibition

El‐Hazek

El-Sabbagh

El-Hazek

et al. 2020

Archiv der Pharmazie

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Generally, highly selective COX-2 inhibitors cause cardiovascular side effects. Celecoxib is the highly marketed coxib, so there is still a need for the synthesis of COX-2 inhibitors with less adverse effects. Moreover, low-dose radiotherapy (LD-RT) is clinically used for the treatment of inflammatory diseases. The present study aimed to investigate the analgesic and anti-inflammatory activity of a novel series of 1,3,4-thiadiazole derivatives alone or combined with LD-RT with a single dose of 0.5 Gy. Initially, in vitro COX-1/COX-2 inhibition assays were performed, identifying the sulfonamide-containing compounds 5-10 as the most potent candidates, with IC 50 values in the range of 0.32-0.37 µM and the highest selectivity indices. These compounds and celecoxib were subjected to in vivo examination after their safety was assessed through the acute toxicity test. Treatment with compounds 5-10 inhibited carrageenan-induced edema by nearly 47-56%, which was nearly equivalent to celecoxib. Compounds 7 and 8 and celecoxib showed an analgesic activity of 64.15%, 49.05%, and 84.90%, respectively, whereas compounds 5, 6, 9, and 10 did not show any analgesic activity unless combined with LD-RT. Ulcerogenic activity, histological paw examination, and docking studies were performed. Compounds 5-10 were nearly similar to celecoxib, showing normal histological features with no ulcerogenic activity.

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Section: Introductionmentioning

confidence: 99%