Nitro adamantane-tetrazole compound, preparing method of nitro adamantane-tetrazole compound and application of nitro adamantane-tetrazole compound
The technology of a compound and tetrazolium, which is applied in the field of medicines for the treatment of diabetes, can solve the problems of undiscovered weight gain and the like
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Embodiment 1
[0019] Example 1 Preparation of Compound I
[0020]
[0021] 2.10g (10mmol) compound II and 3.04g (30mmol) triethylamine were dissolved in 20mL of dry dichloromethane, stirred under ice-water bath cooling, then slowly added dropwise 2.42g (12mmol) compound III dissolved in 5mL of dry dichloromethane solution in methyl chloride. After the addition was complete, the reaction mixture was stirred at room temperature for 1 hour. The reaction mixture was poured into 200 mL of ice water, stirred, extracted with 50 mL×3 dichloromethane, the combined extracts were washed with saline, dried over anhydrous sodium sulfate, and then evaporated to dryness on a rotary evaporator, and the obtained residue was purified by column chromatography , the pure product of IV was obtained, white solid, ESI-MS, m / z=330 and 332 ([M+H] + ).
[0022] 1.97 g (6 mmol) of compound IV 0.68 g (6 mmol) of compound V, 1.00 g (6 mmol) of solid potassium iodide and 4.15 g (30 mmol) of solid potassium carbona...
Embodiment 2
[0024] Example 2 Preparation of Reference Compound D
[0025] In order to fully illustrate the beneficial effects of the compounds of the present invention, the applicant has recorded the following compound D (unpublished) found during the experiment as a pharmacodynamic reference compound.
[0026]
[0027] Its preparation method is as follows:
[0028]
[0029] 1.65g (10mmol) of compound II-1 and 3.04g (30mmol) of triethylamine were dissolved in 20mL of dry dichloromethane, stirred under cooling in an ice-water bath, and then slowly added dropwise 2.42g (12mmol) of compound III dissolved in 5mL of dry solution made in dichloromethane. After the addition was complete, the reaction mixture was stirred at room temperature for 1 hour. The reaction mixture was poured into 200 mL of ice water, stirred, extracted with 50 mL×3 dichloromethane, the combined extracts were washed with saline, dried over anhydrous sodium sulfate, and then evaporated to dryness on a rotary evapor...
Embodiment 3
[0032] Example 3 Determination of the inhibitory effect of compounds on DPP-IV enzymes
[0033] Using the fluorescent DPP4 activity detection kit of BPS Bioscience Company, the inhibitory activity of the compound of the present invention on DPP-IV enzyme was determined.
[0034] Dilute the samples successively according to the concentration of 5, 10, 30, 100 and 200ng / kg, and add the samples in the following table in the fluorescence reaction 96-well plate:
[0035]
[0036] Place in a water bath at 22°C for 10 minutes, use a Spectra Max M5 fluorescence detector with an excitation light of 350nm, and measure the absorbance with 450nm fluorescence. Calculation of IC from the concentration-fluorescence intensity curve 50 values, the results are shown in the table below:
[0037] IC of compounds for inhibition of DPP-IV enzymes 50 value
[0038]
[0039] It can be seen from the above table that the compound of the present invention has a strong inhibitory effect on DPP-...
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