268541-94-2Relevant academic research and scientific papers
Dicationic dithiocarbamate carbapenems with anti-MRSA activity
Imamura, Hideaki,Ohtake, Norikazu,Jona, Hideki,Shimizu, Aya,Moriya, Minoru,Sato, Hiroki,Sugimoto, Yuichi,Ikeura, Chinatsu,Kiyonaga, Hideo,Nakano, Masato,Nagano, Rie,Abe, Shinnosuke,Yamada, Koji,Hashizume, Terutaka,Morishima, Hajime
, p. 1571 - 1578 (2001)
A new class of β-methylcarbapenems bearing a doubly quaternarized 1,4-diazabicyclooctane (DABCO) substituted dithiocarbamate moiety at the C-2 side chain was prepared, and the biological profiles of the compounds, including in vitro and in vivo anti-MRSA activity and DHP-I susceptibility, were evaluated to identify a carbapenem derivative that was superior to BO-3482 (1). As a result, we discovered a 1@β-methyl-2-[4-(4-carbamoylmethyl-1,4-diazabicyclo[2,2,2octanediium-1-yl)methyl-1,2,3,6-tetrahydropyridinylthiocarbonylthio]carbapenem, 14a showing greater than 2-fold better anti-MRSA activity in a mouse infection model and 3-fold better DHP-I susceptibility as compared with BO-3482 (1). Copyright
