US20240118263, Compound Azithromycin BDBM50373918 AZITHROMYCIN Azasite
BDBM27177 triazole-linked azithromycin-based compound, 16a
BDBM27179 triazole-linked azithromycin-based compound, 16c
triazole-linked azithromycin-based compound, 16e BDBM27181
triazole-linked azithromycin-based compound, 16g BDBM27183
triazole-linked azithromycin-based compound, 16h BDBM27184
6-{4-[4-({[(2S,3R,4S,6R)-2-{[(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-1-oxa-6-azacyclopentadecan-11-yl]oxy}-3-hydroxy-6-methyloxan-4-yl](methyl)amino}methyl)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyhexanamide triazole-linked azithromycin-based compound, 16b BDBM27178
7-{4-[4-({[(2S,3R,4S,6R)-2-{[(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-1-oxa-6-azacyclopentadecan-11-yl]oxy}-3-hydroxy-6-methyloxan-4-yl](methyl)amino}methyl)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyheptanamide BDBM27180 triazole-linked azithromycin-based compound, 16d
triazole-linked azithromycin-based compound, 16f BDBM27182 8-{4-[4-({[(2S,3R,4S,6R)-2-{[(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-1-oxa-6-azacyclopentadecan-11-yl]oxy}-3-hydroxy-6-methyloxan-4-yl](methyl)amino}methyl)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyoctanamide
- Surface Plasmon Resonance (SPR) (1) Screening of Macrolide and Cyclic Peptide Drugs by Taking SelH as a TargetA surface plasmon resonance (SPR) method was adopted to detect the interaction condition of a small molecule and a protein, so that the screening of drugs targeting SelH was carried out.1. Protein ImmobilizationPurified SelH was diluted into a 50 μg/mL protein solution by using 10 mM sodium acetate with a pH value of 5.5, the purified SelH was fixed onto a CM5 chip by an amino coupling method by using Biacore 8K (GE Healthcard, Sweden), and an RU value was recorded.2. Sample PreparationThe macrolide compound or cyclic peptide compound (the compounds specifically include carrimycin, isovalerylspiramycin I, spiramycin, carbomycin, azithromycin, erythromycin and thiostrepton) was dissolved in 100% DMSO to be prepared into solutions containing 5% DMSO of different concentrations (0, 31.25, 62.5, 125, 250 and 500 μM) by using a 1.05×PBS-P+ buffer solution (GE Healthcare, obtained by diluting 10×PBS-P+).3. Binding ExperimentA single-cycle kinetics method was adopted, the 1.05×PBS-P+ buffer solution containing 5% DMSO was used as a Running Buffer, different compounds of different concentrations flowed through the SelH fixed onto the chip, wherein the binding time was 120 s, and the change condition of the RU value was recorded. An equilibrium dissociation constant (KD) was calculated by using software in Biacore 8K so as to evaluate the binding affinity between the protein and the compounds.