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Review
. 2024;20(3):311-351.
doi: 10.2174/0115734064253813231025093707.

A Critical Review on Therapeutic Potential of Benzimidazole Derivatives: A Privileged Scaffold

Ramalakshmi Natarajan  1 , Padma Kumar  1 , Arunkumar Subramani  2 , Amuthalakshmi Siraperuman  1 , Prabakaran Angamuthu  1 , Richie R Bhandare  3 , Afzal B Shaik  4   5
Affiliations
Review

A Critical Review on Therapeutic Potential of Benzimidazole Derivatives: A Privileged Scaffold

Ramalakshmi Natarajan et al. Med Chem. 2024.

Abstract

Benzimidazole nucleus is a predominant heterocycle displaying a wide spectrum of pharmacological activities. The privileged nature of the benzimidazole scaffold has been revealed by its presence in most small molecule drugs and in its ability to bind multiple receptors with high affinity. A literature review of the scaffold reveals several instances where structural modifications of the benzimidazole core have resulted in high-affinity lead compounds against a variety of biological targets. Hence, this structural moiety offers opportunities to discover novel, better, safe and highly potent biological agents. The goal of the present review is to compile the medicinal properties of benzimidazole derivatives with a focus on SAR (Structure-Activity Relationships).

Keywords: Benzimidazole; SAR.; lead compounds; multiple targets; privileged scaffold; structure-activity relationship.

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References

    1. Kaur G.; Silakari O.; Benzimidazole scaffold based hybrid molecules for various inflammatory targets: Synthesis and evaluation. Bioorg Chem 2018,80,24-35 - DOI - PubMed
    1. Cozza G.; Girardi C.; Ranchio A.; Lolli G.; Sarno S.; Orzeszko A.; Kazimierczuk Z.; Battistutta R.; Ruzzene M.; Pinna L.A.; Cell-permeable dual inhibitors of protein kinases CK2 and PIM-1: Structural features and pharmacological potential. Cell Mol Life Sci 2014,71(16),3173-3185 - DOI - PubMed
    1. Lavrador-Erb K.; Ravula S.B.; Yu J.; Zamani-Kord S.; Moree W.J.; Petroski R.E.; Wen J.; Malany S.; Hoare S.R.J.; Madan A.; Crowe P.D.; Beaton G.; The discovery and structure–activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia. Bioorg Med Chem Lett 2010,20(9),2916-2919 - DOI - PubMed
    1. Cichero E.; Tonelli M.; Novelli F.; Tasso B.; Delogu I.; Loddo R.; Bruno O.; Fossa P.; Benzimidazole-based derivatives as privileged scaffold developed for the treatment of the RSV infection: A computational study exploring the potency and cytotoxicity profiles. J Enzyme Inhib Med Chem 2017,32(1),375-402 - DOI - PubMed
    1. Ozadali-Sari K.; Tüylü Küçükkılınç T.; Ayazgok B.; Balkan A.; Unsal-Tan O.; Novel multi-targeted agents for Alzheimer’s disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles. Bioorg Chem 2017,72,208-214 - DOI - PubMed

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