苯并咪唑支架作为抗溃疡潜在核心的全面综述

IF 0.7 4区 化学 Q4 CHEMISTRY, ORGANIC Letters in Organic Chemistry Pub Date : 2024-01-25 DOI:10.2174/0115701786267759231121070546
Kuldeep Singh, Bharat Bhushan, Ajit Kumar Varma, Ravi Shekhar, Rajeev Kumar Sharma, Niladry Sekhar Ghosh, Ekta Pandey, Sunam Saha, Shivendra Kumar, Avinash Kumar Mishra, Mohit Agarwal
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引用次数: 0

摘要

:苯并咪唑支架是开发新型溃疡治疗药物的一个很有前景的核心。其独特的化学结构提供了理想的药理特性,如出色的生物利用度、代谢稳定性和低毒性,使其成为治疗溃疡的理想候选药物。在临床前和临床研究中,几种苯并咪唑衍生物已显示出显著的抗溃疡活性,它们通过多种途径发挥作用,包括抑制胃酸分泌、抑制胃部炎症和促进粘膜保护。一些苯并咪唑衍生物还具有抗幽门螺旋杆菌的活性,这表明它们具有消灭与溃疡形成有关的细菌的潜力。然而,溶解性差和选择性有限等挑战依然存在。为了克服这些问题并改善苯并咪唑衍生物的治疗效果,人们探索了各种方法,如原药设计和制剂优化。总之,苯并咪唑支架作为开发新型抗溃疡药物的核心具有广阔的前景。要充分发挥其潜力并将其转化为有效的溃疡治疗方法,还需要进一步的研究和优化工作。随着药物化学和药物设计的不断进步,苯并咪唑类化合物可能会为溃疡和相关胃肠道疾病患者提供新的治疗选择。因此,本综述重点介绍了有关苯并咪唑支架、溃疡形成机制以及各种具有抗溃疡活性的苯并咪唑衍生物的知识,这些知识可在临床前和临床试验中进一步研究。
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A Comprehensive Review of the Benzimidazole Scaffold as a Potential Nucleus for Anti-Ulcer Activity
: The benzimidazole scaffold is a promising nucleus for developing novel therapeutic agents for ulcer treatment. Its unique chemical structure provides desirable pharmacological properties, such as excellent bioavailability, metabolic stability, and low toxicity, making it an attractive candidate for ulcer treatment. Several benzimidazole derivatives have shown significant anti-ulcer activity in preclinical and clinical studies, acting through multiple pathways, including inhibition of gastric acid secretion, suppression of gastric inflammation, and promotion of mucosal protection. Some benzimidazole derivatives have also demonstrated anti-Helicobacter pylori activity, suggesting their potential for eradicating bacteria associated with ulcer formation. However, challenges such as poor solubility and limited selectivity remain. Various approaches, such as prodrug design and formulation optimization, have been explored to overcome these issues and improve the therapeutic profile of benzimidazole derivatives. Overall, the benzimidazole scaffold holds great promise as a nucleus for developing novel anti-ulcer agents. Further research and optimization efforts are needed to harness its full potential and translate it into effective treatments for ulcers. With continued advancements in medicinal chemistry and drug design, benzimidazole-based compounds may offer new therapeutic options for patients suffering from ulcers and related gastrointestinal disorders. Hence, this review highlights the knowledge about benzimidazole scaffold, the mechanism of ulcer formation, and various benzimidazole derivatives with anti-ulcer activity, which can be further studied in pre-clinical and clinical trials.
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来源期刊
Letters in Organic Chemistry
Letters in Organic Chemistry 化学-有机化学
CiteScore
1.30
自引率
12.50%
发文量
135
审稿时长
7 months
期刊介绍: Aims & Scope Letters in Organic Chemistry publishes original letters (short articles), research articles, mini-reviews and thematic issues based on mini-reviews and short articles, in all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is to publish quality papers rapidly by taking full advantage of latest technology for both submission and review of the manuscripts. The journal is an essential reading for all organic chemists belonging to both academia and industry.
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