Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems. Part III:
BIOORGANIC & MEDICINAL CHEMISTRY(1999)
摘要
The synthesis and biological activity of a novel series of 2-alkyl-4-pyrrolidinylthio-beta-methylcarbapenems containing a variety of cationic heteroaromatic substituents is described. As a result of these studies, we uncovered a relationship between in vitro antibacterial activity and the length of the alkyl spacer part, and discovered FR20950 (1c), containing a two methylene spacer moiety and an imidazolio group, which possesses a balanced spectrum of antibacterial activity, including Pseudomonas aeruginosa and Methicillin-resistant Staphylococcus aureus (MRSA). Furthermore, FR20950 exhibited excellent urinary recovery, and comparable stability against renal dehydropeptidase-I (DHP-I) to Biapenem. DHP-I stability could be improved by introduction of a substituent on to the imidazole ring. (C) 1999 Elsevier Science Ltd. All rights reserved.
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关键词
carbapenems,antibacterials,cationic heteroaromatics,DHP-I stability
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