Studies on β-lactam antibiotics. Synthesis and antibacterial activity of novel 1β-methylcarbapenems related to FR21818: 5-membered ring analogs

The synthesis and biological activity of the novel series of 1β-methylcarbapenems 1 are described. Most compounds displayed extremely potent antibacterial activity and high renal DHP-I stability. The best compound in this series, FR21818 ( 1a) displayed excellent in vivo efficacy against an MRSA inf...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-06, Vol.7 (11), p.1409-1414
Main Authors: Azami, Hidenori, Barrett, David, Tanaka, Akira, Sasaki, Hiroshi, Matsuda, Keiji, Sakurai, Minoru, Matsumoto, Yoshimi, Tawara, Shuichi, Chiba, Toshiyuki, Sakane, Kazuo
Format: Article
Language:English
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The synthesis and biological activity of the novel series of 1β-methylcarbapenems 1 are described. Most compounds displayed extremely potent antibacterial activity and high renal DHP-I stability. The best compound in this series, FR21818 ( 1a) displayed excellent in vivo efficacy against an MRSA infection in mice. The synthesis, in vitro antibacterial activity, and stability to human DHP-I of the novel series of carbapenems 1 are described. Most compounds displayed extremely potent activity and the best compound in this series, FR21818 ( 1a), displayed excellent efficacy against a lethal systemic infection by MRSA in mice.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00230-8