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Exenatide analogue with hydroxyamino and application thereof

A technology of exenatide and analogs, applied in the field of medicinal chemistry, can solve problems such as unreported drug properties, and achieve the effects of being beneficial to optimization and development, reducing metabolic inactivation, and prolonging half-life and hypoglycemic effect in vivo.

Active Publication Date: 2018-11-20
JIANGNAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of glycosylation modification strategies to improve the drug properties of Ex4 has not been reported

Method used

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  • Exenatide analogue with hydroxyamino and application thereof
  • Exenatide analogue with hydroxyamino and application thereof
  • Exenatide analogue with hydroxyamino and application thereof

Examples

Experimental program
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Embodiment 1

[0037] 1.1 Lysine analog K with hydroxylamine side chain ＊ Synthesis

[0038] Such as figure 1 As shown, Z-Glu-Obzl (1-benzyl-N-benzyloxycarbonyl-L-glutamic acid) was used as a synthetic lysine analog K ＊ The starting material of , obtain the lysine analogue K containing hydroxylamine side chain through 7 steps reaction ＊ , the total yield was 32.1%. The Fmoc-protected lysine analog K ＊ It can be directly used in solid-phase synthesis of polypeptides.

[0039] The starting material was commercial Z-Glu-OBzl, and Z-Glu-Obzl (22.3 g, 60 mmol) was dissolved in dry THF (150 mL). Add sodium chloride into the ice to make ice salt, adjust the temperature of the ice salt by controlling the amount of sodium chloride added, and adjust the temperature to about -10°C. Place the Z-Glu-OBzl solution on an ice-salt bath at -10°C and stir, then cool and stir for 10 min, and pay attention to prevent water from entering the solution. Add N-methylmorpholine (N-methylmorpholine, 6.6mL, 60m...

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Abstract

The invention discloses an exenatide analogue with hydroxyamino and application thereof and belongs to the field of medical chemistry. The Exendin-4 is modified, and exendin-4 analogues with long pharmacological action time can be obtained. Compared with exenatide, the exenatide analogue disclosed by the invention has the effect of decreasing blood sugar with long pharmacological action time. Synthesis of the target peptide is realized by an orthogonal protection strategy solid-phase synthesis method.

Description

technical field [0001] The invention relates to exenatide analogs with hydroxylamine groups and applications thereof, belonging to the field of medicinal chemistry. Background technique [0002] Diabetes mellitus is a comprehensive metabolic disorder characterized by increased blood sugar levels due to insufficient insulin secretion or defective insulin action in the body. Sustained chronic hyperglycemia will lead to damage, dysfunction and even failure of various tissues and organs, such as eyes, cardiovascular and nerves. With the rapid development of the global economy and the continuous improvement of people's living standards, diabetes has become one of the three major non-communicable diseases that endanger human health. It is estimated that by 2030, there will be more than 300 million people with diabetes worldwide. In my country, the incidence rate of diabetes is as high as 9.7%. In 2010, the total number of diabetic patients reached 92.4 million, becoming the coun...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08B37/00C08B37/08C08H1/00A61K38/22A61P3/10C07K14/575
CPCA61K38/00A61P3/10C07K14/57563C08B37/00C08B37/0072C08G81/00C08H1/00
Inventor 吴志猛周志昉李晨戴士杰刘少中
Owner JIANGNAN UNIV
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