Ohtake N, Yamada K, Mano E, Okamoto O, Ushijima R, Nakagawa S
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
J Antibiot (Tokyo). 1997 Jul;50(7):567-85. doi: 10.7164/antibiotics.50.567.
The synthesis and biological activity of (1R,5S,6S)-2-[(3S,5S)-5-substituted pyrrolidin-3-ylthio]-6-[(R)-1-hydroxyethyl]-1-methyl-1-ca rbapen-2-em-3- carboxylic acid, in which lactams and cyclic amines are introduced as substituents, are described. They showed potent antibacterial activity against Gram-positive and Gram-negative bacteria including P. aeruginosa. Among them, BO-2502A (4h-1) was selected for further evaluation.
描述了(1R,5S,6S)-2-[(3S,5S)-5-取代吡咯烷-3-基硫代]-6-[(R)-1-羟乙基]-1-甲基-1-碳青霉烯-2-烯-3-羧酸的合成及其生物活性，其中内酰胺和环胺作为取代基被引入。它们对包括铜绿假单胞菌在内的革兰氏阳性菌和革兰氏阴性菌显示出强效抗菌活性。其中，BO-2502A(4h-1)被选作进一步评估。
