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CN-120574167-B - Niacin diphenyl diester derivative, preparation and application

CN120574167BCN 120574167 BCN120574167 BCN 120574167BCN-120574167-B

Abstract

The invention belongs to the technical field of medicines, and particularly relates to a nicotinic acid biphenyl diester derivative, a preparation and application, wherein the nicotinic acid biphenyl diester derivative has the following structure: Wherein R 1 、R 2 、R 3 、R 4 、R 5 is independently selected from H, halogen, hydroxy, C1-3 alkyl, C1-3 alkoxy or cyclopropane, at least one of R 1 、R 2 、R 3 、R 4 、R 5 is R, R 6 、R 7 、R 8 、R 9 、R 10 is independently selected from H, halogen, hydroxy, C1-3 alkyl, C1-3 alkoxy or cyclopropane, at least one of R 6 、R 7 、R 8 、R 9 、R 10 is R, R is The invention has the functions of reducing blood fat, reducing blood sugar and resisting bacteria, and has better effect.

Inventors

  • ZHANG JUN
  • ZHENG XING
  • DAI LING

Assignees

  • 湖南科技职业学院

Dates

Publication Date
20260505
Application Date
20250729

Claims (7)

  1. 1. The nicotinic acid biphenyl diester derivative is characterized by being 2,4 '-nicotinic acid biphenyl diester, 3,4' -nicotinic acid biphenyl diester, 4 '-nicotinic acid biphenyl diester, 2,3' -nicotinic acid biphenyl diester, 3 '-nicotinic acid biphenyl diester or 2,2' -nicotinic acid biphenyl diester.
  2. 2. The biphenyl di-nicotinate derivative of claim 1 wherein the biphenyl di-nicotinate derivative is 3,4' -biphenyl di-nicotinate.
  3. 3. A formulation comprising a biphenyldicarboxylate derivative of nicotinic acid as defined in any one of claims 1-2.
  4. 4. A formulation according to claim 3 in the form of a tablet, capsule, pill, granule, syrup, emulsion or suspension.
  5. 5. Use of a biphenyl di-nicotinate derivative according to any one of claims 1-2 for the manufacture of a medicament for reducing blood lipid.
  6. 6. Use of a biphenyl di-nicotinate derivative according to any one of claims 1-2 for the manufacture of a medicament for lowering blood glucose.
  7. 7. Use of a biphenyl di-nicotinate derivative according to any one of claims 1-2 for the preparation of an antibacterial medicament.

Description

Niacin diphenyl diester derivative, preparation and application Technical Field The invention belongs to the technical field of medicines, and particularly relates to a nicotinic acid biphenyl diester derivative, a preparation and application. Background Nicotinic acid is an indispensable nutrient component for human body and plays a very important role in promoting normal growth and development of human body. Nicotinic acid can improve the excitability of central nervous system, protect cardiovascular and cerebrovascular systems, prevent and relieve severe migraine, and reduce cholesterol and triglyceride. Development of nicotinic acid synthesis and application research, wang Jia and the like, anhui chemical industry, 2019,45:13-15, and discloses application of nicotinic acid. CN201210365392.2 discloses a preparation method and application of curcumin ester derivative containing nicotinic acid and acetylsalicylic acid, which have the functions of regulating blood lipid, reducing blood sugar, reducing blood pressure, resisting cancer, resisting inflammation, resisting thrombosis, resisting virus, protecting nervous system and treating senile dementia. Disclosure of Invention The invention aims to solve the technical problem of providing a nicotinic acid diphenyl diester derivative, a preparation and application thereof, and the nicotinic acid diphenyl diester derivative has the effects of reducing blood fat and blood sugar and resisting bacteria, and has a good effect. The embodiment of the invention provides a nicotinic acid biphenyl diester derivative, which has the structure as follows:; Each R 1、R2、R3、R4、R5 is independently selected from H, halogen, hydroxy, C1-3 alkyl, C1-3 alkoxy or cyclopropane, and at least one of R 1、R2、R3、R4、R5 is R; each R 6、R7、R8、R9、R10 is independently selected from H, halogen, hydroxy, C1-3 alkyl, C1-3 alkoxy or cyclopropane, and at least one of R 6、R7、R8、R9、R10 is R; R is 。 Preferably, one of the R 1、R2、R3、R4、R5 is R, and one of the R 6、R7、R8、R9、R10 is R. Preferably, R 1、R2、R3、R4、R5 is independently selected from H, one of R 1、R2、R3、R4、R5 is R, R 6、R7、R8、R9、R10 is independently selected from H, and one of R 6、R7、R8、R9、R10 is R. Preferably, the nicotinic acid diphenyl diester derivative is 2,4 '-nicotinic acid diphenyl diester, 3,4' -nicotinic acid diphenyl diester, 4 '-nicotinic acid diphenyl diester, 2,3' -nicotinic acid diphenyl diester, 3 '-nicotinic acid diphenyl diester or 2,2' -nicotinic acid diphenyl diester. Preferably, the nicotinic acid diphenyl diester derivative is 3,4' -nicotinic acid diphenyl diester. The embodiment of the invention provides a preparation which comprises the nicotinic acid diphenyl diester derivative. Preferably, the formulation is in the form of a tablet, capsule, pill, granule, syrup, emulsion or suspension. The embodiment of the invention provides application of the nicotinic acid biphenyl diester derivative, which is used for preparing a medicament for regulating blood fat. The embodiment of the invention provides application of the nicotinic acid diphenyl diester derivative in preparing a medicament for reducing blood sugar. The embodiment of the invention provides application of the nicotinic acid biphenyl diester derivative, and the nicotinic acid biphenyl diester derivative is used for preparing antibacterial medicines. The preparation method of the nicotinic acid diphenyl diester derivative comprises the step of reacting the diphenyl diphenol and the derivative thereof with nicotinic acid in a solvent at 55-80 ℃ for 2-20 hours to obtain a target product. The solvent is thionyl chloride or acetyl chloride. The nicotinic acid biphenyl diester derivative reacts with acid at the temperature of 5-90 ℃ to obtain the salt of the compound, wherein the acid is hydrochloric acid, hydrobromic acid or hydroiodic acid, and hydrochloric acid is preferred. The invention has the beneficial effects that experiments are carried out on the blood lipid regulating, blood sugar reducing and bacteriostasis performances of each compound, and the experimental results show that the compound 101, the compound 102, the compound 104 or the compound 105 can obviously reduce the plasma LDL-C level, has a certain reduction effect on TG and TC, and simultaneously has the effect of raising HDL-C, and the efficacy is equivalent to lovastatin. Compound 102, compound 103, compound 104 or compound 106 significantly reduced the fasting blood glucose concentration in db/db mice, with efficacy comparable to metformin. Compound 102, compound 103, compound 104 or compound 105 had a remarkable antibacterial effect. The invention also carries out acute toxicity experiments, namely, 1 large dose of the gastric lavage compound 101, the compound 105 and the compound 106 is used for mice, indexes such as behavior activity and the like of the mice and the toxicity reaction degree are continuously observed, and the mice are sacrificed for carrying out the caesarean decomposition at the