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О проекте
Two synthetic pathways for conjugates of clarithromycin (active against Gram positive infections) and congeners of 1-hydroxy-1,3-dihydrobenzoxa[2,1][c]borol (effective for Gram negative microbes) are elaborated. Clarithromycin and benzoxa[2,1][c]borol derivatives are the ligands of bacterial RNA. First pathway explored the substitution of the C-9 carbonyl group of clarithromycin, the second direction used the modification of the 4’’-O-group of cladinose via formation of carbamates of benzoxaborols. The last one was more successful and 4”-O-(3-S-(1-hydroxy-1,3-dihydro-benz[c][1,2]oxaborole)-methyl-carbamoyl-clarithromycin showed twofold decrease in MICs for S. epidermidis and S. pneumoniae than clarithromycin. 4’’-O-Modified clarithromycins demonstrated an efficacy against Gram positive strains only. Compounds with C-9 substitution were more active than 4’’-O-substituted antibiotics only for susceptible strains E. coli tolC and did not exceed activity of initial antibiotics.
Научная область
P Two approaches to the use of bezo[c][1,2]oxaboroles as active fragments for synthetic transformation of clarithromycin
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