Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, 147002, India.
Molecular Modelling Lab (MML), Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, 147002, India.
Eur J Pharmacol. 2021 May 15;899:174027. doi: 10.1016/j.ejphar.2021.174027. Epub 2021 Mar 14.
The fused heterocyclic ring system has been recognized as a privileged structure that is used as a template in medicinal chemistry for drug discovery. Benzimidazole is one of the common scaffolds found in several natural products such as histidine, purines, and an integral part of vitamin B12. This hetero-aromatic bicyclic ring system acts as a pharmacophore in various drugs of therapeutic interest and has a broad spectrum of activity. Literature reports suggest that diversely substituted benzimidazoles possess distinct pharmacological profiles with multi-targeting potential, thereby, an indispensable anchor for the development of novel therapeutic agents against complex diseases such as cancer, malaria, inflammatory disorders, microbial diseases, hypertension, etc. Thus, lots of efforts have been diverted towards exploring the therapeutic potential of benzimidazoles. Despite great efforts made by the research community, still, some multi-factorial diseases continue to progress due to their complex pathophysiology. Under these sets of circumstances, there is a need to explore this nucleus for hybrid designing with multi-targeting potential against complex diseases. Benzimidazole-based hybrids have been reported to treat multifactorial diseases, making it a scaffold of interest for various pharmaceutical companies and research groups. In this write-up, we shed light on the recent pharmacological profiles, various designing strategies, and structure-activity relationships (SAR) of different benzimidazole-based hybrids.
稠合杂环体系已被认为是一种重要的结构,可作为药物化学中药物发现的模板。苯并咪唑是几种天然产物(如组氨酸、嘌呤)中常见的支架之一,也是维生素 B12 的组成部分。这个杂芳族双环体系在各种具有治疗意义的药物中充当药效团,具有广泛的活性。文献报道表明,具有不同取代基的苯并咪唑具有独特的药理学特性和多靶点潜力,因此是开发针对癌症、疟疾、炎症性疾病、微生物疾病、高血压等复杂疾病的新型治疗药物的不可或缺的关键。因此,人们投入了大量精力来探索苯并咪唑的治疗潜力。尽管研究界做出了巨大努力,但由于其复杂的病理生理学,一些多因素疾病仍在继续发展。在这种情况下,有必要探索这种核,以获得针对复杂疾病的多靶点潜力的混合设计。基于苯并咪唑的杂合体已被报道可用于治疗多种因素疾病,因此成为各大制药公司和研究团队关注的支架。在这篇综述中,我们介绍了苯并咪唑类杂合体的最新药理学特性、各种设计策略和构效关系 (SAR)。