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A derivative, genipin technology, applied in the field of preparation of new compounds
Active Publication Date: 2013-03-27
HERBALIFE LEISHUO HUNAN NATURAL PROD
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[0009] No further studies on other genipin derivatives and their antidiabetic activity in the prior art
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Embodiment 1
[0133] The synthesis of embodiment 1 genipin derivative
[0134] 1.1 Instruments and reagents
[0135] Nuclear magnetic resonance spectrum adopts Brucker 400MHz ADVANCE DMX 500 type nuclear magnetic resonance instrument to measure (TMS is internal standard, CDC1 3 is solvent); mass spectrum adopts Esquire 600 (Germany Brucker) mass spectrometer to measure (ESI-MS);
[0136] Genipin was purchased from Linchuan Zhixin Biotechnology Co., Ltd.; the silica gel was 200-300 mesh (Qingdao Ocean Chemical Factory), and other reagents were domestic analytical reagents without further purification before use.
[0137] 1.2 Synthesis of intermediates
[0138] Synthesis of Intermediate 1: Add genipin (5g, 22.1mmol), methanol (100mL), and boron trifluoride ether (500mg) into a 500mL single-necked bottle, stir at room temperature for 24h, and monitor by TLC. After the reaction is complete, add saturated Sodium bicarbonate quenched the reaction, removed most of the methanol under reduced pre...
Embodiment 2
[0171] Example 2 Detection of anti-diabetic biological activity of genipin derivatives
[0172] The peroxisome proliferator-activated receptor gamma subtype is a fatty acid receptor that plays a key role in energy metabolism. Dysfunction of the peroxisome proliferator-activated receptor gamma subtype is associated with diabetes, cardiovascular disease, and obesity, and this receptor is therefore an important target for the development of drugs for type II diabetes. However, the experimental data show that the compound of the present application has no activating effect on the peroxisome proliferator-activated receptor gamma subtype.
[0173] Dipeptidyl peptidase IV inhibitors are new hypoglycemic drugs that have attracted much attention at present. Studies have shown that dipeptidyl peptidase IV inhibitors can promote the release of insulin from β cells, increase the synthesis of insulin in β cells, and inhibit the secretion of glucagon at the same time, without hypoglycemia ...
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Abstract
The invention belongs to the field of preparation of new compounds and in particular provides a genipin derivative as well as a preparation method and an application thereof. The genipin derivative and pharmaceutically acceptable salt thereof are shown as a general formula I (described in the specification), wherein R1 is one selected from C1-6 alkyl or alkyl amino, C1-20 aryl, C1-20 aromatic amino and C1-6 heterocyclic amino; R2 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle and an amino group; R3 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle, methylsulfonyl, p-tosyl group and -COR4, and R4 is one selected from C1-6 alkyl, C1-20 aryl, C1-6 heterocycle and the amino group. The derivative provided by the invention has application value in preparation of medicine used for treating diabetes mellitus II.
Description
technical field [0001] The field of preparation of novel compounds of the present invention relates to genipin derivatives and their uses. Background technique [0002] According to statistics from the World Health Organization in 2011, the number of diabetic patients worldwide has reached 366 million, the vast majority of which are type 2 diabetes, and about 4.6 million people die of the disease and its complications every year. The main drugs currently used to treat diabetes are sulfonylureas, thiazolidinediones and metformin. However, for many patients, these drugs make it difficult to maintain blood sugar at a normal level. Therefore, it is of great significance to invent a new type of drug to treat diabetes. [0003] Traditional Chinese medicine has a certain effect on the prevention and treatment of type II diabetes. Chinese traditional Chinese medicine uses gardenia flower extract to treat the symptoms of type II diabetes, which can achieve obvious thirst-quenching...
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