A NOVEL 1-BETA-METHYLCARBAPENEM ANTIBIOTIC, S-4661 SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2-(5-SUBSTITUTED PYRROLIDIN-3-YLTHIO)-1-BETA-METHYLCARBAPENEMS

Authors
ISO Y IRIE T NISHINO Y MOTOKAWA K NISHITANI Y
Citation
Y. Iso et al., A NOVEL 1-BETA-METHYLCARBAPENEM ANTIBIOTIC, S-4661 SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2-(5-SUBSTITUTED PYRROLIDIN-3-YLTHIO)-1-BETA-METHYLCARBAPENEMS, Journal of antibiotics, 49(2), 1996, pp. 199-209
Citations number
8
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
49
Issue
2
Year of publication
1996
Pages
199 - 209
Database
ISI
SICI code
0021-8820(1996)49:2<199:AN1ASS>2.0.ZU;2-I
Abstract
The synthesis and biological activity of(1R,5S,6S)-2-[(3S,5S)-5-substi tuted 1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acids are des cribed. These compounds exhibit potent antibacterial activity against a wide range of both Gram-positive and Gram-negative bacteria includin g Pseudomonas aeruginosa. Of these new carbapenems, (1R,5S,6S)-2-[(3S, 5S)-5-sulfamoylaminomethyl 1-hydroxyethyl]-1-methylcarbapen-2-em-3-car boxylic acid (S-4661) showed the most potent and well balanced activit y and was selected as a candidate for further evaluation.