Kamachi H, Oka M, Narita Y, Iimura S, Aburaki S, Yamashita H, Tomatsu K, Okumura J, Naito T
Bristol-Myers Research Institute, Ltd., Tokyo Research Center, Japan.
J Antibiot (Tokyo). 1990 May;43(5):533-43. doi: 10.7164/antibiotics.43.533.
The synthesis and antimicrobial activity of eight derivatives of 7-[(Z)-2-(2-aminothiazol-4-yl)- and 7-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoacetamido] cephalosporins having an (E) or (Z)-3-ammonio-1-propenyl group in the C-3 side chain are described. The (E)-propenyl derivatives were more active than their corresponding Z-isomers and showed well-balanced, broad antibacterial activity against both Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.
描述了8种7-[(Z)-2-(2-氨基噻唑-4-基)-和7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧基亚氨基乙酰胺基]头孢菌素衍生物的合成及其抗菌活性，这些衍生物在C-3侧链上具有(E)或(Z)-3-铵基-1-丙烯基。(E)-丙烯基衍生物比其相应的Z-异构体更具活性，并且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均表现出平衡的广谱抗菌活性。
