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L-p-nitrophenylalanine amide dipeptide derivative and its preparation method and application

A technology of nitrophenylalanine amide and peptide derivatives, which is applied in the field of drug synthesis and can solve problems such as indigestion, inability to effectively improve diabetes lipid metabolism disorder, liver toxicity and the like

Active Publication Date: 2020-07-24
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there are many types of diabetes treatment drugs, but long-term use will cause side effects such as liver toxicity, weight gain, edema, and indigestion to varying degrees, and generally cannot effectively improve the lipid metabolism disorder associated with diabetes

Method used

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  • L-p-nitrophenylalanine amide dipeptide derivative and its preparation method and application
  • L-p-nitrophenylalanine amide dipeptide derivative and its preparation method and application
  • L-p-nitrophenylalanine amide dipeptide derivative and its preparation method and application

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Embodiment Construction

[0037] In order to make the object, technical solution and beneficial effect of the present invention clearer, preferred embodiments of the present invention will be described in detail below.

[0038] 1. Synthesis of L-p-nitrophenylalaninamide dipeptide derivatives

[0039] 1. Synthesis of Intermediate I

[0040]

[0041] Under ice bath, add 20mmol of L-p-nitrophenylalanine and saturated Na to the reaction flask 2 CO 3 Aqueous solution 50mL, stirred in an ice bath until dissolved, slowly drop into the dissolved (Boc) 2 O 24mmol of acetone solution 10mL, after stirring for 1h, transfer to a 35-55°C water bath to stir the reaction, keep the pH of the reaction solution at 8-9, monitor by thin-layer chromatography (TLC) until the reaction is completed. Under the condition of pH about 10, the reaction solution was extracted with diethyl ether (30mL×2), the pH of the aqueous phase was adjusted to 3-5 with 3N HCl, and then extracted with ethyl acetate (EA) (30mL×3). phase, wa...

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Abstract

The invention discloses an L-p-nitro phenylalaninamide dipeptide derivative having a following structure formula. Results of in-vitro antidiabetic activity tests show that most compounds have the agonist activity of PPAR (peroxisome proliferators activated receptors); the agonist rate of individual compounds relative to rosiglitazone PPRE (peroxisome proliferators activated receptor response elements) is as high as 270.96 percent; EC50 reaches 0.4380mu g / ML; all of the compounds can be used for preparing antidiabetic medicines. The potential application prospects are achieved in the diabetes treatment field. The formula of the compound is shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and relates to a class of L-p-nitrophenylalaninamide dipeptide derivatives, and also relates to its preparation method and application in pharmacy. Background technique [0002] Diabetes mellitus (DM) is an endocrine and metabolic disease caused by the absolute or relative insufficiency of the body's insulin and the decreased sensitivity of cells to insulin. Major social issues that threaten human health. At present, there are many types of diabetes treatment drugs, but long-term use will cause side effects such as liver toxicity, weight gain, edema, and indigestion to varying degrees, and generally cannot effectively improve the lipid metabolism disorder associated with diabetes. Therefore, the research and development of novel anti-diabetic drugs with high efficiency and low toxicity is still an important task in the prevention and treatment of diabetes. [0003] Peroxisome prolife...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/072C07K1/02C07K1/06A61K38/05A61P3/10
CPCA61K38/00C07K5/06104Y02P20/55
Inventor 杨大成唐雪梅范莉李元元冯计周刘红芳张利刘滨
Owner SOUTHWEST UNIV
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