Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity

El‐Nezhawy, Ahmed O. H.; Biuomy, Ayman R; Hassan, Fatma S. M.; Ismaiel, Ayman K.; Omar, Hany A.

doi:10.1016/j.bmc.2013.01.070

Cited by 51 publications

(36 citation statements)

References 28 publications

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“…Immediately thereafter, the rats received 100 mL of vehicle or carrageenan (1% in saline) s.c. on the plantar surface of the left hind paw under mild anesthesia, essentially, as reported before 21 . The paw edema was evaluated by measuring paw-volume changes at 1, 3 and 6 h after carrageenan injection using a plethysmometer.…”

Section: Carrageenan-induced Rat Paw Edema Assaymentioning

confidence: 85%

3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

Abdellatif¹,

Lamie²,

Omar

2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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In a new group of 3-methyl-2-phenyl-1-substituted-indole derivatives (10a-f), the indomethacin analogs were prepared via the Fisher indole synthesis reaction of propiophenone with appropriately substituted phenylhydrazine hydrochloride. This is followed by the insertion of the appropriate benzyl or benzoyl fragment. All the synthesized compounds were evaluated for their anti-inflammatory (in vitro and in vivo) and analgesic activities. The methanesulphonyl derivatives 10d, e and f showed the highest anti-inflammatory (in vitro and in vivo) and analgesic activities. In addition, molecular docking studies were performed on compounds 10a-f and the results were in agreement with that obtained from the in vitro COX inhibition assays. The significant anti-inflammatory and analgesic activities exhibited by 10d and 10e warrant continued preclinical development as potential anti-inflammatory and analgesic agents.

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Section: Carrageenan-induced Rat Paw Edema Assaymentioning

confidence: 85%

3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

Abdellatif¹,

Lamie²,

Omar

2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Most of the chemokines, which were found to be modulated in the present study, can activate members of the transmembrane receptor family TREM. activity (10) and omeprazole was shown to possess additional antiinflammatory activity (8,16,17), this comparison should identify targets not related to acid suppression.…”

Section: Factor Analysis Identified Cinc1-3 Mip-1/3` Mig Rantes Anmentioning

confidence: 99%

GPR84 and TREM-1 Signaling Contribute to the Pathogenesis of Reflux Esophagitis

Abdel-Aziz

Schneider

Neuhuber

et al. 2015

Mol Med

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Gastro-esophageal reflux disease (GERD) is one of the most common disorders in gastroenterology. Patients present with or without increased acid exposure indicating a nonuniform etiology. Thus, the common treatment with proton pump inhibitors (PPIs) fails to control symptoms in up to 40% of patients. To further elucidate the pathophysiology of the condition and explore new treatment targets, transcriptomics, proteomics and histological methods were applied to a surgically induced subchronic reflux esophagitis model in Wistar rats after treatment with either omeprazole (PPI) or STW5, a herbal preparation shown to ameliorate esophagitis without affecting refluxate pH. The normal human esophageal squamous cell line HET-1A and human endoscopic biopsies were used to confirm our findings to the G-protein-coupled receptor (GPR) 84 in human tissue. Both treatments reduced reflux-induced macroscopic and microscopic lesions of the esophagi as well as known proinflammatory cytokines. Proteomic and transcriptomic analyses identified CINC1-3, MIP-1/3α, MIG, RANTES and interleukin (IL)-1β as prominent mediators in GERD. Most regulated cyto-/chemokines are linked to the TREM-1 signaling pathway. The fatty acid receptor GPR84 was upregulated in esophagitis but significantly decreased in treated groups, a finding supported by Western blot and immunohistochemistry in both rat tissue and HET-1A cells. GPR84 was also found to be significantly upregulated in patients with grade B reflux esophagitis. The expression of GPR84 in esophageal tissue and its potential involvement in GERD are reported for the first time. IL-8 (CINC1-3) and the TREM-1 signaling pathway are proposed, besides GPR84, to play an important role in the pathogenesis of GERD.

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“…Immediately thereafter and under light anesthesia, the animals received 100 ml of vehicle or carrageenan (1% in saline) s.c. on the plantar surface of the left hindpaw as reported before 22,23 . The development of paw edema was assessed by measuring pawvolume changes at 1, 3 and 6 h after carrageenan injection using plethysmometer.…”

Section: Carrageenan-induced Rat Paw Edema Assaymentioning

confidence: 80%

Synthesis, characterization and biological evaluation of novel 4′-fluoro-2′-hydroxy-chalcone derivatives as antioxidant, anti-inflammatory and analgesic agents

Abdellatif

Elshemy

Salama

et al. 2014

Journal of Enzyme Inhibition and Medicinal Chemistry

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In an effort to develop safe and potent anti-inflammatory agents, a series of novel 4 0 -fluoro-2 0 -hydroxychalcones 5a-d and their dihydropyrazole derivatives 6a-d was prepared. It was synthesized via aldol condensation of 4 0 -fluoro-2 0 -hydroxyacetophenone with appropriately substituted aldehydes followed by cyclization with hydrazine hydrate. All the synthesized compounds were evaluated for their antioxidant, anti-inflammatory, cyclooxygenase inhibition selectivity and analgesic activities. The dimethoxychalcone 5a and its dihydropyrazole derivative 6a showed the highest antioxidant activity, while the monomethoxychalcone 5d and its dihydropyrazole derivative 6d showed the highest analgesic and anti-inflammatory activities. It was also found that there is a close correlation between 4 0 -fluoro-2 0 -hydroxychalcones 5a-d and their dihydropyrazole derivatives 6a-d in the screened biological activities. To explain the correlation between the synthesized chalcones and their dihydropyrazole derivatives, especially for the anti-inflammatory activity, docking studies were performed.

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Design, synthesis and pharmacological evaluation of omeprazole-like agents with anti-inflammatory activity

Cited by 51 publications

References 28 publications

3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

GPR84 and TREM-1 Signaling Contribute to the Pathogenesis of Reflux Esophagitis

Synthesis, characterization and biological evaluation of novel 4′-fluoro-2′-hydroxy-chalcone derivatives as antioxidant, anti-inflammatory and analgesic agents

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