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Tetrazole carboxylic acid compounds and application thereof

A compound and application technology, applied in the field of peroxisome proliferator-activated receptor agonists, can solve problems such as obvious side effects and weight gain

Inactive Publication Date: 2015-01-21
ZHEJIANG PHARMA COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PPARγ is considered to be the main molecular target of glitazone insulin sensitizers. Although glitazones are effective drugs for the treatment of type II diabetes, the side effects of these compounds are very obvious, such as severe liver toxicity, weight gain and anemia, which is mainly due to the fact that glitazones are the main or complete agonists of PPARγ (N · Ajie, D · Rocher, S · Yvonne, CN101098865A)

Method used

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  • Tetrazole carboxylic acid compounds and application thereof
  • Tetrazole carboxylic acid compounds and application thereof
  • Tetrazole carboxylic acid compounds and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022]

[0023]

[0024] 2.70g (10mmol) compound A-1 and 1.24g (10mmol) compound B-1 are dissolved in 10mL DMF, add 4.15g (30mmol) K 2 CO 3 , and then stirred overnight at 120 °C under nitrogen protection. The reaction mixture was cooled slightly and poured into 100mL of ice water, stirred, adjusted to pH=3-4 with concentrated hydrochloric acid, extracted with 50mL×3 dichloromethane, combined the extract phases, washed once with brine, dried over anhydrous sodium sulfate, and evaporated on a rotary evaporator. The solvent was evaporated to obtain a residue, and then purified by column chromatography to obtain the pure product of C-1, ESI-MS, m / z=331 ([M+NH 4 ] + ).

[0025] Dissolve 2.50g (8mmol) of compound C-1 in 10mL of dry toluene, stir slowly under cooling in an ice-water bath, and slowly add 2.71g (10mmol) of PB r3 Dissolve in 2 mL of dry dichloromethane solution. After the dropwise addition, the reaction mixture was stirred at room temperature for half an hour...

Embodiment 2-5

[0028] According to the method of Example 1, the compounds of general formula I shown in the table below were prepared.

[0029]

[0030]

Embodiment 6

[0032] The sample was formulated with 1% sodium carboxymethylcellulose into a suspension at a concentration of 5 mg / mL, and the administration volume was 0.4 mL / 20 g of body weight, equivalent to a dose of 100 mg / kg.

[0033] Healthy ICR mice, half male and half male, weighing 20-24g, meet the first-class standard. Animals were fasted for 16 hours, given the compound to be tested by intraperitoneal injection of 2g / kg glucose saline solution for 15 minutes after intraperitoneal injection, and were regularly taken from the retrobulbar venous plexus of mice at 0.5h, 1h, 1.5h and 2h after modeling. Blood was centrifuged to separate serum, and the serum glucose content at each time point was determined by glucose oxidase method. Blank mice received neither glucose nor

[0034] The compound to be tested was given, and the model mice were only given glucose without the compound to be tested.

[0035]

[0036] It can be seen from the data in the above table that each administrati...

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Abstract

The invention relates to the field of diabetes related medicines. The invention particularly relates to tetrazole-carboxylic-acid-containing compounds (disclosed as general formula I) capable of treating diabetes as a peroxisome proliferator-activated receptor (PPAR) agonist, and a preparation method and application thereof in treating diabetes. In the general formula I, the groups are defined in the specification.

Description

technical field [0001] The invention relates to the field of medicine related to diabetes. Specifically, the present invention relates to a class of peroxisome proliferator-activated receptor (PPAR) agonists containing a tetrazolium carboxylic acid skeleton that has a therapeutic effect on diabetes, its preparation method and pharmaceutical compositions containing them . Background technique [0002] Diabetes mellitus is a disease in which the patient's ability to control blood sugar is impaired, and the patient has lost, to varying degrees, the ability to respond appropriately to the action of insulin. Most of diabetes is type II diabetes (non-insulin-dependent diabetes), accounting for about 80%-90%. Studies have found that insulin resistance in peripheral tissues (including skeletal muscle, liver and adipose tissue, etc.) , development plays an extremely important role. A class of drugs that sensitize patients to their own insulin, insulin sensitizers, has been introdu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D257/04A61K31/41A61P3/10A61P9/00A61P3/04
Inventor 郭章华
Owner ZHEJIANG PHARMA COLLEGE
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