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Review Paper | Medicine Science | Volume 15 Issue 7, July 2026 | Pages: 187 - 199 | India
Synthesis, Pharmacological Activities, Structure-Activity Relationship of Benzimidazole-Indole Conjugates: A Review
Abstract: Benzimidazole-indole conjugates have emerged as an important class of heterocyclic hybrids exhibiting remarkable structural diversity and potent biological activities. The combination of two privileged pharmacophores-benzimidazole and indole- within a single molecular framework enhances their physicochemical properties, target selectivity, and therapeutic potential. Numerous synthetic methodologies have been explored to obtain these conjugates efficiently, including one-pot cyclo-condensation, Suzuki-Miyaura coupling, N-alkylation, base hydrolysis, Claisen-Schmidt condensation, cyclization, domino Sonogashira cyclization, Steglich-type esterification, Knoevenagel condensation, and Fischer indole synthesis. These strategies provide access to a wide variety of benzimidazole-indole scaffolds with diverse substitution patterns under mild and environmentally compatible conditions. Structure-activity relationship (SAR) studies reveal that substitutions on the benzimidazole N1 position and the indole C? or C5 positions significantly influence anticancer, antimicrobial, antitubercular, and diuretic activities. The conjugation of electron-withdrawing or lipophilic substituents generally enhances biological potency by improving membrane permeability and receptor binding affinity. This review comprehensively summarizes the synthetic strategies, mechanistic pathways, and pharmacological profiles of benzimidazole-indole conjugates, emphasizing their potential as lead compound for novel medicinal product development.
Keywords: Benzimidazole, Benzimidazole-indole conjugate, indole core-compounds, synthetic approach, structure activity relationship (SAR), biological activities
How to Cite?: Upasana Sharma, Sadhana Sharma, Dimple Dimple, "Synthesis, Pharmacological Activities, Structure-Activity Relationship of Benzimidazole-Indole Conjugates: A Review", Volume 15 Issue 7, July 2026, International Journal of Science and Research (IJSR), Pages: 187-199, https://www.ijsr.net/getabstract.php?paperid=SR26702103634, DOI: https://dx.doi.org/10.21275/SR26702103634