Application of alkaloids or salts thereof in anti-coronavirus
A coronavirus and alkaloid technology, applied in the direction of antiviral agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as drugs that have not obtained new coronaviruses, and achieve excellent coronavirus suppression effects and high suppression active effect
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preparation example 1
[0035] This preparation example is used to illustrate the preparation of the compound represented by formula (S, R-2-1).
[0036]
[0037] The compound represented by formula (S, R-2-1) is prepared according to the above reaction process.
[0038] (1) Preparation of compound 2
[0039] N 2 Under protection, add 1.14 g (0.03 mol) NaBH in batches to 150 mL of freshly distilled anhydrous THF at room temperature 4 , add 6.84 grams (0.02mol) of raw material 1 (purchased from Bailingwei Technology Co., Ltd.) in batches under stirring, stir for 10 minutes, slowly add 6.99 grams (0.03mol) of zirconium tetrachloride, stir at room temperature for 10 hours, and TLC detects that the reaction of raw materials is complete . Add 10mL of water and 10mL of dilute hydrochloric acid dropwise under cooling in an ice-water bath to fully decompose excess NaBH 4 , after precipitation with 250mL CH 2 Cl 2 Dilute with 50mL of water, stir and separate, the organic phase is washed with water, w...
Embodiment 1
[0056] The following will evaluate the inhibitory effect of the compound represented by formula (S, R-2-1) on the new coronavirus 2019-nCoV through multiple concentration gradient experiments at the cell level.
[0057] (1) Dilute the new coronavirus 2019-nCoV (from virus isolation) with DMEM, so that the titer of the new coronavirus 2019-nCoV is 100TCID 50 / 100μL maintenance solution. The maintenance solution was prepared by adding 2% serum (Gibco) and double antibodies (penicillin and streptomycin) to DMEM (Gibco) medium.
[0058] (2) Dilute the compound (10 mM) represented by the formula (S, R-2-1) 10-fold stepwise with maintenance solution to different concentrations (5 μM, 0.5 μM, 0.05 μM, 0.005 μM, 0.0005 μM, 0.00005 μM) The solution to be tested, the volume of each concentration is 900 μL; Remdesivir (Remedsivir, purchased from Gilead Sciences) was gradually diluted to different concentrations (100 μM, 20 μM, 4 μM, 0.8 μM, 0.16 μM, 0.032 μM) of the solution to be test...
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