Paper Report for: Nandha_2018_Arch.Pharm.(Weinheim)_351_e1800030
Reference
Title: Synthesis of substituted fluorobenzimidazoles as inhibitors of 5-lipoxygenase and soluble epoxide hydrolase for anti-inflammatory activity Nandha B, Ramareddy SA, Kuntal H Ref: Arch Pharm (Weinheim), 351:e1800030, 2018 : PubMed
A new series of 4-((5-fluoro-6-(substituted)-1H-benzo[d]imidazol-2-ylthio)methyl)-benzoic acids 4a-o and 2-(5-fluoro-6-(substituted)-1H-benzo[d]imidazol-2-ylthio)-2-methylpropanoic acids 8a-e were synthesized, and their inhibitory potencies against soluble epoxide hydrolase (sEH) and 5-lipoxygenase (5-LOX) were investigated. These molecules were designed based on the combination of 5-LOX and sEH pharmacophores, resulting in hybrid analogs with potent sEH and 5-LOX inhibitory activity. Compound 4g showed remarkable activity with IC50 values of less than 1 muM (0.9 muM) against 5-LOX, while compound 4k displayed promising activity against sEH with IC50 </= 1 muM (0.7 muM). These compounds were evaluated for their in vivo potential using the carrageenan-induced rat paw edema assay. Based on the obtained results, the structure-activity relationship was established and a correlation between the activities was observed. Compounds 4f, 4g, 4k, 4n, and 8e showed potent anti-inflammatory activity and significant inhibition of edema (64.13, 67.39, 66.30, 65.21, and 58.69%, respectively) at a dose of 100 mg/kg, comparable to the standard drug ibuprofen (70.65%) at 3 h.
        
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Nandha B, Ramareddy SA, Kuntal H (2018) Synthesis of substituted fluorobenzimidazoles as inhibitors of 5-lipoxygenase and soluble epoxide hydrolase for anti-inflammatory activity Arch Pharm (Weinheim)351: e1800030
Nandha B, Ramareddy SA, Kuntal H (2018) Arch Pharm (Weinheim)351: e1800030