Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives

Abstract

Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-α and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new imidazopyridines with potential therapeutic effects in acute inflammatory diseases.

Design and Synthesis of Benzodiazepines Bearing Benzimidazole/Benzothiazole and Indole Moieties as a Potent Antimicrobial and Antioxidant Agents

“…It has been found to possess antioxidant, anti-inflammatory, diuretic, antiviral, anticonvulsant, and antidiabetic [12][13][14][15][16][17] activities.…”

Copper-incorporated fluorapatite encapsulated iron oxide nanocatalyst for synthesis of benzimidazoles

“…Benzimidazole is an important structural moiety which is present in many natural and synthetic compounds with a variety of interesting biological activities [1], such as anticancer [2], antiarrhythmic [3], antihistaminic [4], antiulcerative [5], antihypertensives, antiviral, antitumor [1], antibacterial, antifungals [6], anti-inflammatory [7], anticonvulsant, antidiabetic properties [8], and antidepressant [9]. The first benzimidazole was described by Hobrecker in 1872, who obtained 2,5 (or 2,6)-dimethylbenzimidazole by the reduction of 2-nitro-4-methylacetanilide [10].…”

Synthesis of benzimidazole derivatives as potent β-glucuronidase inhibitors

“…Derivatives of benzimidazole have been associated with wide range of biological activities including anti-cancer [22], anti-glycation [23], anti-inflammatory [24], anti-urease [25], anti-fungals [26], anti-bacterials [27], anti-helminthes [28], proton pump inhibitors [29], anti-virals [30], anti-oxidants [31], anti-hypertensives [32], carbonic anhydrase inhibitors [33], phosphodiesterase inhibitor [34] and anti-coagulants [35].…”