Chemical and Pharmaceutical Bulletin p. 2326 - 2330 (1996)
Update date:2022-07-29
Topics:
Lee, Hong-Woo
Kim, Eung-Nam
Son, Hoe-Joo
Ahn, Soon-Kil
Chung, Koo-Hun
Kim, Jung-Woo
Lee, Chong-Ryoul
A series of new carbapenem derivatives, which have a pyrrolidin-4-ylthio group substituted with a hydroxyalkyl or carbamoyl group at the 2′ position as the C-2 side chain, have been prepared. The antibacterial activity and the stability to renal dehydropeptidase-I of these compounds were investigated, and the structure-activity relationships were studied. Among these new carbapenems, (1R,5S,6S)-2-[(2S,4S)-2-{(2-hydroxy)ethylmercaptomethyl}pyrrolidin-4-ylthio]-6- [(1R)-1-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylic acid (1a) showed the most potent and well balanced activity and was selected as a candidate for further evaluation.
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Doi:10.1007/BF00906003
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