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In this study ten new compounds Sd-01-Sd-10 were synthesized via acylation from sitagliptin and various fatty acyl chlorides. Animal experiments approved by the Institutional Animal Care and Use Committee of Jilin Provincial Institute of Pharmaceutical Research (approval No. 2025001). The target compounds were evaluated for their in vivo hypoglycemic activity using a type 2 diabetic mouse model, with subsequent structure-activity relationship analysis and further assessment of the most active compounds via an oral glucose tolerance test. Meanwhile, a maximum feasible dose test was conducted in healthy mice for preliminary safety evaluation. The results indicated that this series of compounds exhibited promising hypoglycemic activity and a high level of safety, which was supported by the observation of no abnormal behavior or mortality in healthy mice after a single oral dose of 2 000 mg·kg-1. Among them, Sd-06 showed activity comparable to sitagliptin, whereas Sd-05 was more potent. Notably, Sd-05 at the lower dose of 30 mg·kg-1 effectively improved glucose tolerance in normal mice, surpassing the efficacy of sitagliptin at 50 mg·kg-1, highlighting its value for further development.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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