Ghani Usman
Clinical Chemistry Unit, Department of Pathology, College of Medicine, King Saud University, Riyadh 11461, Saudi Arabia.
Eur J Med Chem. 2015 Oct 20;103:133-62. doi: 10.1016/j.ejmech.2015.08.043. Epub 2015 Aug 28.
Treatment of diabetes mellitus by oral α-glucosidase inhibitors is currently confined to acarbose, miglitol and voglibose marred by efficacy problems and unwanted side effects. Since the discovery of the drugs more than three decades ago, no significant progress has been made in the drug development area of anti-diabetic α-glucosidase inhibitors. Despite existence of a wide chemical diversity of α-glucosidase inhibitors identified to date, majority of them are simply piled up in publications and reports thus creating a haystack destined to be forgotten in the scientific literature without given consideration for further development into drugs. This review finds those "needles" in that haystack and lays groundwork for highlighting promising α-glucosidase inhibitors from the literature that may potentially become suitable candidates for pre-clinical or clinical trials while drawing attention of the drug development community to consider and take already-identified promising α-glucosidase inhibitors into the next stage of drug development.
目前，口服α-葡萄糖苷酶抑制剂治疗糖尿病仅限于阿卡波糖、米格列醇和伏格列波糖，这些药物存在疗效问题和不良副作用。自三十多年前发现这些药物以来，抗糖尿病α-葡萄糖苷酶抑制剂的药物开发领域一直没有取得重大进展。尽管迄今为止已鉴定出的α-葡萄糖苷酶抑制剂具有广泛的化学多样性，但它们中的大多数只是堆积在出版物和报告中，因此在科学文献中形成了一个注定会被遗忘的干草堆，而没有考虑进一步开发成药物。本综述在那个干草堆中找到那些“针”，并为突出文献中可能成为临床前或临床试验合适候选药物的有前景的α-葡萄糖苷酶抑制剂奠定基础，同时引起药物开发界的关注，以考虑将已鉴定出的有前景的α-葡萄糖苷酶抑制剂推进到药物开发的下一阶段。
