Flavane (isoflavane) urease inhibitor and synthesis and use thereof
A technology of isoflavane and flavan, applied in the field of preparation of anti-gastritis and gastric ulcer medicines, can solve the problems of instability and distortion of phosphoric acid diamides
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Embodiment 1
[0061] Embodiment 1: the preparation of 5,7-dihydroxyflavan
[0062] Dissolve 2.54g of chrysin in 70mL of ethanol, and stir magnetically at room temperature. After dissolving, add 80mg of 5% Pd∕C (20% water content), and react at room temperature for 4h. TCL tracking shows that the reaction is complete. Filter and recover Pd∕C, and concentrate the filtrate After purification by column chromatography on silica gel (200-300 mesh) (AcOEt:petroleum ether=1:2), 2.14g of white solid was obtained with a yield of 88%. Mp 262-264℃; EIMS m / z: 242 [M + ];IR(KBr)cm -1 :3575(OH); 1 H NMR (DMSO- d 6 ) δppm: 2.48 (t, 2H), 2.59 (m, 2H), 4.79 (t, 1H), 6.47 (d, 1H), 6.63 (d, 1H), 6.75 (m, 5H), 7.61 (s, 1H ), 8.02(s, 1H).
Embodiment 2
[0064] According to the method similar to Example 1, using flavones (isoflavones) in different substitution forms as raw materials, the flavans (isoflavanes) listed in Table 1 and Table 2 were synthesized 1 ~ 32 .
[0065] Table 1 General formula Ⅱ Each R group of the flavan
[0066] serial number R 1 R 2 R 3 R 4 R 5 R 6 R 7 R 8 1 H Oh H H Oh H H H 2 H Oh H Oh Oh H H H 3 H Oh H Oh H H Oh Oh 4 H Oh Oh H Oh H H H 5 H Oh Oh H H Oh Oh H 6 H Oh Oh H H H Oh Oh 7 H Oh Oh H H H H Oh 8 H Oh Oh Oh Oh H H H 9 H Oh Oh Oh Oh H Oh H 10 H Oh Oh Oh Oh H Oh Oh 11 H Oh Oh Oh Oh Oh H H 12 H Oh Oh Oh Oh H H Oh 13 H Oh Oh Oh Oh Oh Oh H 14 H Oh Oh Oh Oh Oh Oh Oh 15 H OMe H OMe H H OMe OMe 16 H ...
Embodiment 3
[0069] Embodiment 3: the inhibitory enzyme activity of compound
[0070] Add 25 μL of Jack bean urease (4U) and 25 μL (1 mM) of the test compound solution to the 96-well plate, incubate at 37 °C for 2 h, then add 55 μL of phosphate buffer containing 100 mM urea and 100 mM, Incubate at 30°C for 15 min, add 45 μL of phenol reagent (mixed solution containing 1% phenol and 0.005% sodium nitroprusside) and 70 μL alkali reagent (mixed solution of NaOCl containing 0.5% NaOH and 0.1% active chlorine), and After standing at room temperature for 50 min, measure the OD value at 630 nm with a microplate reader, and the percentage inhibition rate is calculated according to the following formula:
[0071]
[0072] All experiments were performed in solutions at pH 8.2 (0.01M K 2 HPO 4 , 1mM EDTA, 0.01M LiCl), the level of activity is measured by the half-inhibition rate IC 50 to indicate that the IC 50 The smaller the value, the higher the activity of the compound. The results are s...
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