CP0569, a new broad-spectrum injectable carbapenem. Part 1: synthesis and structure-activity relationships.

  title={CP0569, a new broad-spectrum injectable carbapenem. Part 1: synthesis and structure-activity relationships.},
  author={Kazuhiro Aihara and Yuko Kano and Sohjiro Shiokawa and Toshiro Sasaki and Fumihito Setsu and Yumiko Sambongi and Miyuki Ishii and K. Tohyama and Takashi Ida and Atsushi Tamura and Kunio Atsumi and Katsuyoshi Iwamatsu},
  journal={Bioorganic \& medicinal chemistry},
  volume={11 16},
9 Citations

Synthesis and evaluation of novel 2,4-disubstituted arylthiazoles against T. brucei

2-{2-[3-(1-Adamantyl)-4-fluorophenyl]thiazol-4-yl}ethan-1-amine and 2-{1-adamantyl)phenyl[4-(2-adammyantyl)]thiazolin[4- phenyl]-thiazolate exhibit activity against T. brucei in the range of IC50 = 0.42 μM and 0.80 μM.

Resistance to β-lactam antibiotics

  • K. Poole
  • Biology, Chemistry
    Cellular and Molecular Life Sciences CMLS
  • 2004
Approaches for overcoming resistance mechanisms include the development of novel β-lactamase-stable β- lactams, β-Lactam enzyme inhibitors to be employed with existing β- Lactamams, compounds that bind strongly to low-affinity PBPs and agents that potentiate the activity of existing β -lactams against low-Affinity PBP-producing organisms.

Concise total synthesis of largazole

The concise total synthesis of largazole was accomplished. The key step included the use of the Nagao thiazolidinethione auxiliary for the diastereoselective acetate aldol reaction and it acts as an



Structure-activity relationships in the 2-arylcarbapenem series: synthesis of 1-methyl-2-arylcarbapenems.

The labile tert-butyldimethylsilyl esters of the azetidinones 6-8b served as the crucial synthons in the preparation of the potentially useful ylide pyridyl thio esters 18-20. These intermediates

The synthesis of 2-(functionalized methyl)-1 beta-methylcarbapenems.

The synthesis of 1 beta-methylcarbapenems having a ROCH2 substituent at the 2-position is described. Their in vitro antibacterial activity and DHP-I susceptibilities are presented.

Formation of imidazopyridines by the phase transfer catalyzed reaction of .alpha.-(aminomethyl)pyridines and CHCl3 with alkaline hydroxide

The reaction of chloroform with 2-(aminomethyl) pyridine (1) under basic phase-transfer catalysis affords the highly fluorescent imidazo [1,5-a] pyridine (2) in 25% isolated yield. The basic phase