A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether: Synthesis and structure–activity relationships (2)
摘要:
A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and its analogues were prepared, and their antibacterial activities and pharmacokinetic properties were evaluated. We found that the introduction of all (R)-alkyl group between the amide and iminoether groups could improve the pharmacokinetic properties while maintaining the activity against erythromycin-resistant Streptococcus pneumoniae. Among the ketolides prepared with the (R)-alkyl group, compound 5p with an N-(3-quinoxalin-6-yl-propyl)-propionamide moiety was found to have in vivo efficacy comparable to CAM with potent in vitro antibacterial activities against the key respiratory pathogens including Haemophilus influenzae and erythromycin-resistant S. pneumoniae. (c) 2006 Elsevier Ltd. All rights reserved.
A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether: Synthesis and structure–activity relationships (2)
摘要:
A new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and its analogues were prepared, and their antibacterial activities and pharmacokinetic properties were evaluated. We found that the introduction of all (R)-alkyl group between the amide and iminoether groups could improve the pharmacokinetic properties while maintaining the activity against erythromycin-resistant Streptococcus pneumoniae. Among the ketolides prepared with the (R)-alkyl group, compound 5p with an N-(3-quinoxalin-6-yl-propyl)-propionamide moiety was found to have in vivo efficacy comparable to CAM with potent in vitro antibacterial activities against the key respiratory pathogens including Haemophilus influenzae and erythromycin-resistant S. pneumoniae. (c) 2006 Elsevier Ltd. All rights reserved.
10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE
申请人:Sugimoto Tomohiro
公开号:US20110152239A1
公开(公告)日:2011-06-23
The present invention relates to a process for preparing compositions of high concentrations of omega-3 fatty acids from krill. Furthermore, the invention relates to a composition comprising high concentrations of omega-3 fatty acids, and a lipid fraction from krill comprising high amounts of the fatty acids with chain length C14 and C 16.
10A-AZALIDE COMPOUND CROSSLINKED AT 10A- AND 12-POSITIONS
申请人:Sugimoto Tomohiro
公开号:US20110237784A1
公开(公告)日:2011-09-29
A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even
Hemophilus influenzae
, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
10A-AZALIDE COMPOUND CROSSLINKED AT POSITION-10A AND POSITION-12
申请人:Taisho Pharmaceutical Co. Ltd.
公开号:EP2177526A1
公开(公告)日:2010-04-21
A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even Hemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).