An insight on medicinal attributes of 1,2,3- and 1,2,4-triazole derivatives as alpha-amylase and alpha-glucosidase inhibitors.

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Molecular Diversity Pub Date : 2024-10-01 Epub Date: 2023-09-21 DOI:10.1007/s11030-023-10728-1
Anushka Sharma, Rahul Dubey, Ritu Bhupal, Preeti Patel, Sant Kumar Verma, Savas Kaya, Vivek Asati
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引用次数: 0

Abstract

Diabetes Mellitus (DM) is the globe's common leading disease which is caused by high consumption of glucose. DM compiles groups of metabolic disorders which are characterized by inadequate secretion of insulin from pancreas, resulting in hyperglycemia condition. Many enzymes play a vital role in the metabolism of carbohydrate known as α-amylase and α-glucosidase which is calcium metalloenzyme that leads to breakdown of complex polysaccharides into glucose. To tackle this problem, search for newer antidiabetic drugs is the utmost need for the treatment and/or management of increasing diabetic burden. The inhibition of α-amylase and α-glucosidase is one of the effective therapeutic approaches for the development of antidiabetic therapeutics. The exhaustive literature survey has shown the importance of medicinally privileged triazole specifically 1,2,3-triazol and 1,2,4-triazoles scaffold tethered, fused and/or clubbed with other heterocyclic rings structures as promising agents for designing and development of novel antidiabetic therapeutics. Molecular hybrids namely pyridazine-triazole, pyrazoline-triazole, benzothiazole-triazole, benzimidazole-triazole, curcumin-triazole, (bis)coumarin-triazole, acridine-9-carboxamide linked triazole, quinazolinone-triazole, xanthone-triazole, thiazolo-triazole, thiosemicarbazide-triazole, and indole clubbed-triazole are few examples which have shown promising antidiabetic activity by inhibiting α-amylase and/or α-glucosidase. The present review summarizes the structure-activity relationship (SAR), enzyme inhibitory activity including IC50 values, percentage inhibition, kinetic studies, molecular docking studies, and patents filed of the both scaffolds as alpha-amylase and alpha-glucosidase inhibitors, which may be used for further development of potent inhibitors against both enzymes.

Abstract Image

对1,2,3-和1,2,4-三唑衍生物作为α-淀粉酶和α-葡萄糖苷酶抑制剂的药用特性的深入了解。
糖尿病(DM)是全球常见的主要疾病,由高血糖摄入引起。糖尿病合并了一组代谢紊乱,其特征是胰腺胰岛素分泌不足,导致高血糖状态。许多酶在碳水化合物的代谢中起着至关重要的作用,称为α-淀粉酶和α-葡萄糖苷酶,这是一种钙金属酶,可将复杂的多糖分解为葡萄糖。为了解决这个问题,寻找新的抗糖尿病药物是治疗和/或管理糖尿病负担增加的迫切需要。抑制α-淀粉酶和α-葡萄糖苷酶是开发抗糖尿病疗法的有效治疗方法之一。详尽的文献调查表明,与其他杂环结构连接、融合和/或俱乐部化的药物特权三唑,特别是1,2,3-三唑和1,2,4-三唑支架,作为设计和开发新型抗糖尿病疗法的有前途的试剂,具有重要意义。分子杂化物,即哒嗪三唑、吡唑啉三唑、苯并噻唑三唑、苯并咪唑三唑、姜黄素三唑、(双)香豆素三唑、吖啶-9-羧酰胺连接的三唑、喹唑啉酮三唑、黄酮三唑,噻唑并三唑,氨基硫脲三唑,吲哚棒状三唑是少数几个通过抑制α-淀粉酶和/或α-葡萄糖苷酶而显示出有前景的抗糖尿病活性的例子。本综述总结了这两种支架作为α-淀粉酶和α-葡萄糖苷酶抑制剂的结构-活性关系(SAR)、酶抑制活性(包括IC50值)、抑制百分比、动力学研究、分子对接研究和专利申请,可用于进一步开发针对这两种酶的强效抑制剂。
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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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