166947-15-5Relevant academic research and scientific papers
Anhydrolide macrolides. 2. Synthesis and antibacterial activity of 2,3- anhydro-6-O-methyl 11,12-carbazate erythromycin A analogues
Griesgraber, George,Kramer, Mark J.,Elliott, Richard L.,Nilius, Angela M.,Ewing, Patty J.,Raney, Patti M.,Bui, Mai-Ha,Flamm, Robert K.,Chu, Daniel T.W.,Plattner, Jacob J.,Or, Yat Sun
, p. 1660 - 1670 (2007/10/03)
A series of 3-descladinosyl-2,3-anhydro-6-O-methylerythromycin A 11,12- cyclic carbazate analogues was prepared and evaluated for antibacterial activity. These 2,3-anhydro macrolides were found to be potent antibacterial agents in vitro against macrolide-susceptible organisms including Staphylococcus aureus 6538P, Streptococcus pyogenes EES61, and Streptococcus pneumoniae ATCC6303. These compounds were also very active against some organisms that show macrolide resistance (S. aureus A5177, S. pyogenes PIU2584, and S. pneumoniae 5649). The compounds generally showed poor activity against organisms with constitutive MLS resistance. Selected compounds were evaluated in vivo in mouse protection studies. Although most of the compounds tested in vivo showed poor efficacy, two compounds, 38 and 57, were more active than clarithromycin against S. pneumoniae ATCC6303.
Erythromycin derivatives
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, (2008/06/13)
A compound selected from the group consisting of a compound of the formula STR1 wherein R1 and R2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form STR2 and R'1 and R'2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.
