Recent Advances in Synthetic α‐Glucosidase Inhibitors

Abstract

Over the past few years, the number of people diagnosed with type 2 diabetes has increased owing to an unhealthy diet, a limited amount of exercise, and obesity. The search for novel and efficient antidiabetes agents has become an urgent task for scientists. Among the antidiabetes drugs, α-glucosidase inhibitor drugs have been proven to have many advantages over other drugs, and therefore, a large number of new compounds as α-glucosidase inhibitors has recently been reported. In this review, we summarize these newly found α-glucosidase inhibitors and their structure-activity relationships in antidiabetic studies and provide better structures for α-glucosidase inhibitors or even preclinical candidates. Beyond that, some enlightening strategies for the synthesis of relevant compounds are highlighted.

Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles

“…To confirm its green chemistry character, we calculated that the atom economy and atom efficiency of the synthesis of 4a are respectively of 92.9 and 47.4%. 13 The reaction had only moderate overall yield but it was nevertheless remarkably effective given that it generated five new bonds (~90% average yield per bond formation). Further mechanistic and synthetic studies on this new three-component reaction are underway.…”

Alpha Glucosidase Inhibitory Activities of Plants with Focus on Common Vegetables

“…Recent studies on the beneficial health effects of vegetables have piqued the interest of researchers due to their possible protection against chronic diseases. In addition, continuous effort is being made in the research and discovery of new anti-glucosidase/anti-diabetic drugs with higher safety profiles for long-term therapy [12][13][14]. Thus, it is worth reviewing the effects of common vegetables for the purpose of identifying novel/potential compounds that may be suitable for development as anti-diabetes agents.…”

From synthetic control to natural products: a focus on N‐heterocycles

“…32,57 Taking into account the amazing diversity of enzymes that could be inhibited by iminosugars, and the scientific tendency and effort to develop the perfect inhibitor for a specific enzyme, a huge number of compounds have been synthesized and tested over the past 50 years. 61 (2R,3R,4R)-(+)-Fagomine 51 (Scheme 7) is a 1,2-dideoxyazasugar isolated from Castanospermum australe (Leguminosae) 62,63 and the seeds of Japanese buckwheat (Fagopyrum esculentum; Polygonaceae). 62,64 It has a strong anti-hyperglycaemic effect in streptozocin-induced diabetic mice and in the potentiation of glucose-induced insulin secretion.…”

“…Taking into account the amazing diversity of enzymes that could be inhibited by iminosugars, and the scientific tendency and effort to develop the perfect inhibitor for a specific enzyme, a huge number of compounds have been synthesized and tested over the past 50 years …”