2-Substituted azole derivatives. 1. Synthesis and antiinflammatory activity of some 2-(substituted-pyridinyl)benzimidazoles

Abstract

A series of 2-(2-pyridinyl)benzimidazoles was synthesized and evaluated for antiinflammatory activity by the carrageenan-induced rat paw edema assay. Among several active derivatives, 2-(5-ethylpyridin-2-yl)benzimidazole (6) was selected for further study. A comparison of compound 6 with phenylbutazone and tiaramide revealed that 6 possesses stronger activity in acute inflammatory models possibly with slightly less gastrointestinal irritation than both phenylbutazone and tiaramide.

Simple, Efficient, and Applicable Route for Synthesis of 2-Aryl(Heteroaryl)-Benzimidazoles at Room Temperature Using Copper Nanoparticles on Activated Carbon as a Reusable Heterogeneous Catalyst

“…These compounds exhibit a wide spectrum of biological and pharmacological activities [1][2][3][4][5][6][7]. Also, 2-aryl benzimidazole derivatives are fluorescent acid-base indicators [8], dopants for plastic scintillation applications [9] and subunits of polybenzimidazoles as thermally stable polymers [10].…”

Structure-Based Design of Benzimidazole Sugar Conjugates: Synthesis, SAR and In Vivo Anti-inflammatory and Analgesic Activities

“…For these reasons, they gained much attention as important pharmacophore and privileged structure in medicinal chemistry [6,7] encompassing a diverse range of biological activities including antibacterial [8,9], anti-parasitic agent [10], antihistamine [11,12], antiulcerative [13], antioxidant [14], antiallergic [15], anticancer activities [16], anti-HIV-1 [17], anti-herpes (HSV-1) [18], and for the treatment of Hepatitis C and B viruses [19,20]. Finally, 2-substitutd benzimidazoles [21,22] and other benzimidazole derivatives [23][24][25] were reported to exhibit anti-inflammatory and analgesic properties. Thus, the unique structural features and pharmaceutical activities of benzimidazoles have encouraged us to synthesize novel 2-methyl-N-substituted benzimidazolesugar conjugates and study their anti-inflammatory and analgesic activities.…”

1-Benzyl-2-Phenylbenzimidazole (BPB), a Benzimidazole Derivative, Induces Cell Apoptosis in Human Chondrosarcoma through Intrinsic and Extrinsic Pathways

“…They have a wide range of biological and pharmacological activities with therapeutic potential. Substituted benzimidazole derivatives have different therapeutic applications, including anti-histamine [12], anti-ulcerative [13], anti-inflammatory [14], anti-oxidant [15], anti-HIV-1 [16], anti-bacterial [17] and anti-cancer activities [18]. We previous reported that benzimidazole derivatives (FPipTB and MPTB) induced cell apoptosis in chondrosarcoma cells [19,20].…”