Benzimidazole–Oxadiazole Hybrids—Development in Medicinal Chemistry: An Overview

Aug 18, 2024Chemical biology & drug design

Overview of Developing Benzimidazole-Oxadiazole Compounds in Medicine

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Abstract

Benzimidazole-oxadiazole hybrids have been identified as the most potent agents for various therapeutic applications.

Combining two or more pharmacophores into a single molecule may enhance pharmacological potency beyond the individual effects.
Heterocyclic compounds, such as benzimidazole and oxadiazole, are crucial for numerous biological activities.
Molecular hybridization can potentially improve drug-like properties, including pharmacokinetics and pharmacodynamics.
The review highlights the biological properties of benzimidazole-oxadiazole hybrids, including anticancer, antimicrobial, and anti-inflammatory effects.
Potential structure-activity relationships and mechanisms of action for these hybrids are discussed to guide future drug design.

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To increase the success rate of drug discovery, one practical strategy is to begin molecular hybridisation. The presence of two or more pharmacophores in a single unit leads to a pharmacological potency greater than the sum of each individual moiety's potency. Heterocyclic compounds are very widely distributed in nature and are essential for life activities. Benzimidazole and oxadiazole are privileged structures in medicinal chemistry and are widely used in drug discovery and development due to their vast biological properties. The drug-like properties (like pharmacokinetics and pharmacodynamics) of the individual scaffolds can be improved by benzimidazole-oxadiazole chimeric molecules via a molecular hybridisation approach. Benzimidazole and oxadiazole cores can either be fused or incorporated using either functional groups/bonds. Over the last few decades, drug discovery scientists have predicted that these moieties could be interconnected to yield a novel or modified hybrid compound. Benzimidazole and oxadiazole hybrids were identified as the most potent anticancer, antimicrobial, anti-inflammatory, antioxidant, anticonvulsant, antidepressant, antihypertensive and antitubercular agents. In this context, the present review describes the biological properties of benzimidazole-oxadiazole (1,3,4 and 1,2,4) hybrids, their possible structure-activity relationship and the mechanism of action studies presented. This review article is intended to stimulate fresh ideas in the search for rational designs of more active and less toxic benzimidazole-oxadiazole hybrid prospective therapeutic candidates, as well as more effective diagnostic agents and pathologic probes.

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Benzimidazole–Oxadiazole Hybrids—Development in Medicinal Chemistry: An Overview

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