A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Abstract

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

Structure–Activity Relationship of New Chimeric Analogs of Mastoparan from the Wasp Venom Paravespula lewisii

“…Taking this into account, we designed and synthesized a series of new TP10 conjugates with RIP or [Lys 2 , Ile 4 ] RIP attached to its C -terminus or benzimidazole derivatives ( Figure 1 ) attached via a methylenecarbonyl linker to the ε-amino side chain group of Lys 7 residue. Benzimidazoles are of great interest due to their broad spectrum of biological activity, including antimicrobial, antiviral and anticancer properties [ 39 , 40 , 41 , 42 , 43 , 44 ].…”

An Efficient Method for Synthesis of New Tricyclic Benzimidazoles by Using Sodium Metabisulphite Adsorbed on Silica and Their Antimicrobial Studies

“…The precursor (4) was synthesized in two steps, in the first step 2-amino-3-nitrophenol (1) reacted with 1,2-dibromoethane (2) in presence of KOH to get 5-nitro-3,4-dihydro-2Hbenzo[b] [1,4]oxazine (3) and in the second step, the nitro group of (3) is reduced in presence of palladium on carbon under hydrogen atmosphere to afford (4) (Scheme 1).…”

“…Imidazole and benzimidazole compounds are well known for their biological activity [1,2] and pharmacological properties. [3] Their biological activity changes when they are fused with another heterocycle to make bicyclic or tricyclic imidazoles. [4] Various tricyclic benzimidazoles [5][6][7][8][9] were synthesized and studied in detail in the last two decades .…”

Benzimidazole‐carbamate anthelmintics: Perspective candidates for the anticancer drug development

“…To counter the solubility issue, several diverse class of derivatives based on benzimidazole‐carbamate scaffold have been developed, however, it still remains challenging to achieve conclusive findings for the structural features and physicochemical properties needed for specific bioactivity of benzimidazole‐carbamates (http://db.idrblab.net/ttd/ttd-search/drug-similarity). In many cases, these challenges led to the discontinuation of further studies on specific benzimidazole‐carbamates for the development of anticancer drugs (Brishty et al, 2021).…”