Novel dithiocarbamate carbapenems with anti-MRSA activity

被引:26
作者
Ohtake, N [1 ]
Imamura, H [1 ]
Jona, H [1 ]
Kiyonaga, H [1 ]
Shimizu, A [1 ]
Moriya, M [1 ]
Sato, H [1 ]
Nakano, M [1 ]
Ushijima, R [1 ]
Nakagawa, S [1 ]
机构
[1] Banyu Pharmaceut Co Ltd, Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan
关键词
D O I
10.1016/S0968-0896(98)00069-8
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A new series of 1 beta-methyl carbapenems, in which a disubstituted-aminothiocarbonylthio moiety was attached to the C-2 position of the carbapenem nucleus, were prepared and evaluated for anti-MRSA activity. These derivatives showed good in vitro antibacterial activity against high-level MRSA, and the finding of good affinity for PBP-2' supported these results. Some of the compounds having favorable protein-binding affinity showed excellent in vivo anti-MRSA activity. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1089 / 1101
页数:13
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