Benzimidazole: A Milestone in the Field of Medicinal Chemistry

Abstract

In the last 2-3 decades, the broad research in the application of benzimidazole derivatives made it important for mankind. Many scientists have worked on benzimidazole derivatives and they found that this compound has a diverse role in the field of medicinal chemistry. Few benzimidazole derivatives are currently in the market as a drug candidate against various diseases. Moreover, the benzimidazole derivatives exhibit pharmacological activities such as anti-tuberculosis, anti-malarial, antihistamine, antimicrobial, antiviral, antidiabetic, anticancer, anti-fungal, anti-inflammatory, analgesic, anti-HIV, etc. In this review, we have summarized various derivatives of benzimidazole which have been prepared by many researchers to understand the chemistry as well as diverse pharmacological activities. These findings may lead the scientists who are working in the field of medicinal chemistry to the development of benzimidazole based drug candidates in the future.

Benzimidazoles in Drug Discovery: A Patent Review

“…Over the years, benzimidazole and its derivatives have been extensively studied in the pharmaceutical field for a wide range of pharmacological activities, which are useful for drug development. Some of the pharmacological activities which have been reported include anti‐cancer, analgesic, anti‐histamine, anti‐inflammatory, anti‐acetylcholinesterase, anti‐fungal, anti‐tubercular, anti‐viral, anti‐malarial and anti‐protozoal [1–12] . Some benzimidazole‐based drugs which have been marketed are as shown in Figure 1.…”

“…Many reviews on benzimidazoles have been published over the years [3,11,12] . Some of them are clearly dated and with new emerging information, comprehensive review of this important class of compounds is desired.…”

Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives

“…[3] Benzimidazole scaffold is present in various pharmacologically active molecules such as bendamustine, omeprazole, telmisartan, lansoprazole, rabeprazole, pantoprazole, mebendazole, albendazole, pimobendam, triclabendazole, and nocodazole ( Figure 1). [4,5] In this view, the incorporation of benzoyl group into benzimidazole can enhance their lipophilicity, bioavailability, and thereby increase the biological potency. [6] Benzimidazole derivatives comprise a auspicious group of heterocyclic derivatives having a large number of pharmaceutical activities such as antimicrobial, [7][8][9][10] antiprotozoal, [11] anthelmintic, [12][13][14] anticancer, [15][16][17] anti-HIV, [18] anticonvulsant, [19] anti-inflammatory, [20] antineoplastic, [21] antiulcer, [22] antiviral, [23][24][25] antihypertensive, [26,27] antitubercular, [28,29] antiulcer activity, [30] anti-histaminic [31] and anti-oxidant.…”

“…[ 3 ] Benzimidazole scaffold is present in various pharmacologically active molecules such as bendamustine, omeprazole, telmisartan, lansoprazole, rabeprazole, pantoprazole, mebendazole, albendazole, pimobendam, triclabendazole, and nocodazole (Figure 1). [ 4,5 ] In this view, the incorporation of benzoyl group into benzimidazole can enhance their lipophilicity, bioavailability, and thereby increase the biological potency. [ 6 ]…”

Synthesis and crystal structures of N-H, N-phenyl and N-benzyl-2-(4-hexyloxyphenyl)benzimidazoles

“…1. Chemical context 2-Arylbenzimidazoles have attracted considerable attention as biologically active compounds (Vasava et al, 2020). They are also used as ligands in constructing cyclometalated iridium(III) and ruthenium(II) complexes for organic lightemitting diodes and photosensitizers in dye-sensitized solar cells (Bezzubov et al, 2020;Lavrova et al, 2020).…”