Norvancomycin-type dimer derivative, preparation method and medicinal application thereof
A technology of norvancomycin, dimer, applied in the field of medicine, to achieve the effect of high antibacterial activity
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Embodiment 1
[0025] Synthesis of norvancomycin dimer derivative 1a
[0026]
[0027] Lead compound 2a (100mg, 0.062mmol) was added to a 25mL three-neck flask, dissolved in 5mL DMF, and after the temperature was lowered to 0°C, DIEA (16.03mg, 0.124mmol) and 0.1% equivalent of CuSO were added 4 .5H 2 O as a catalyst, under nitrogen protection, TfN was added dropwise at 0 °C 3 The DCM solution was added to the reaction system, and reacted at 0°C for 8h. TLC monitors that the basic reaction of the raw materials is complete. Slowly add DCM dropwise to the system, gradually insoluble matter is produced, continue to drop DCM until no insoluble matter is produced, centrifuge, discard the supernatant, and obtain lavender powdery solid 3a (92 mg , yield 90.7%);
[0028] Add compound 3a (100mg, 0.061mmol) into a 10mL three-neck flask, dissolve it with 5mL DMF, add DIEA (31.6mg, 0.244mmol), after compound 3a is completely dissolved, N 2 Add bridge chain I (8mg, 0.0305mmol) and 0.1% CuI under pr...
Embodiment 2
[0039] The test of embodiment 2 in vitro antibacterial activity
[0040] Adopt the final product (1) a-c of embodiment 1 to carry out the test of in vitro bacteriostatic activity; Concrete method carries out antimicrobial drug minimum inhibitory concentration determination (Minimal Inhibitory concentration MIC) to carry out;
[0041] Take 1ml of antibacterial drugs of different types and different concentrations and pour them into 9cm sterile empty plates, then immediately pour 19ml of sterile M-H agar cooled to about 55°C on the plates, and mix well with the liquid to make the culture medium antibacterial drugs The final concentrations were 128, 64, 32, 16, 8, 4, 2, 1, 0.5, 0.25, 0.125, 0.06 μg / ml; at the same time, M-H plates without antibacterial drugs were prepared as controls; bacterial inoculations were incubated for 18 hours The bacteria were added to sterile normal saline with an inoculation needle to prepare a bacterial solution with a concentration of 0.5 McFarland ...
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