A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

Abstract

Background: Benzimidazole is a category of heterocyclic aromatic compounds formed from the fusion of six membered benzene with five membered imidazolering. The moiety possesses diverse biological and clinical applications. A number of studies have shown that a varied substituent around the benzimidazole nucleus results in pharmacologically active compounds of therapeutic interest. Purpose: Owing to its number of pharmacological properties, this moiety is of choice of interest in designing and synthesis of new therapeutic compounds. The existence of the benzimidazole core in numerous groups of biological agents like antimicrobial, antiviral, antiparasitic, antihypertensive, anticancer, CNS stimulant as well as depressants has made important scaffold for development of many newer therapeutic agents. There is utmost need to understand the synthesis and associated role of benzimidazole derived compounds in different diseases. Therefore, in the present review, we attempt to discuss various derivatives of benzimidazole nucleus with different pharmacological activities. Conclusion: Benzimidazoles have played a great role in discovery of drug and development. Huge attempt has been made towards benzimidazole heterocyclic-based organic compounds with great excellence that resulted in drugs with enormous biological activity. Therapeutic drugs containing benzimidazole nucleus are used in building drugs that serve to be an active area of research. This article becomes a source that will lead to discovery of new opportunities for all researchers interested in benzimidazole-based heterocyclic medicinal chemistry.

Synthesis and Investigation of the Anticancer Activities of Platin Complexes Bearing 2,5(6)-Disubstitutedbenzimidazole Derivative Ligands

“…Literatür taramalarında benzimidazol halkasının 1, 2 ve 5 numaralı konumları sübstitüe edilerek farklı hastalıkların tedavisi için molekül tasarlama çalışmalarının yapıldığı görülmektedir [23][24][25][26][27][28][29][30][31][32][33]. Bu çalışmada da benzimidazol halkasının 5 numaralı konumunda F/Cl/CH3 ve 2 numaralı konumunda da H/CH3 sübstitüenti bulunan altı adet 5(6)-floro/kloro/metil-2-hidrojen/metilbenzimidazol türevleri Philips yöntemi kullanılarak sentezlenmiştir [34]…”

“…Heteroaromatik bisiklik halka sistemine sahip olan benzimidazol, yapısında bulunan asidik ve bazik özelliğe sahip azot atomlarından dolayı amfoterik karakter göstermektedir. DNA yapı taşını oluşturan pürin bazlarına, birçok kofaktör, aminoasitler ve vitamin B12 gibi biyoaktif moleküllerinin yapısında bulunmasından dolayı organizmanın tanıdığı aromatik bir halka sistemidir [22][23][24][25]. Benzimidazol halka sistemine sahip ilaçların antikanser, antihelmintik, antifungal, antiviral, antienflamatuvar, antihistaminik, antipsikotik gibi terapötik etkinlikleri bulunmaktadır [25][26][27][28][29][30].…”

Novel Benzo[4,5]imidazo[1,2-a]pyrimidine derivatives as selective Cyclooxygenase-2 Inhibitors: Design, synthesis, docking studies, and biological evaluation

“…According to recent studies, the COX-2 inhibitors with tricyclic rings as central skeletons are introduced [ 19 – 21 ]. Benzimidazole rings have been appeared as the prominent scaffold in medicinal chemistry and also used as the central core in COX-2 inhibitors [ 22 – 28 ]. Our previous work introduced a new potent and selective COX-2 inhibitors class with tricyclic benzimidazole central core (A, Fig.…”