Mochida K, Shiraki C, Yamasaki M, Hirata T, Sato K, Okachi R
J Antibiot (Tokyo). 1987 Jan;40(1):14-21. doi: 10.7164/antibiotics.40.14.
A series of new carbacephem compounds which have substituted aminothiazolylglycyl side chain have been prepared starting from corresponding carbacephems with aminothiazolylmethoxyimino group. Among them, the compound having 3,4-dihydroxybenzoyl group showed very sharp activity against Pseudomonas aeruginosa. Moreover, the optical resolution of alpha carbon of aminothiazolylglycyl moiety was carried out through preparation of optically active side chain and the (S)-isomer (KT-4380) was found to be the most active against Pseudomonas sp. as well as other Gram-negative strains.
从具有氨噻唑基甲氧基亚氨基的相应碳头孢烯出发，制备了一系列具有取代氨噻唑基甘氨酰侧链的新型碳头孢烯化合物。其中，具有3,4 - 二羟基苯甲酰基的化合物对铜绿假单胞菌显示出极强的活性。此外，通过制备旋光活性侧链对氨噻唑基甘氨酰部分的α-碳进行了旋光拆分，发现（S）-异构体（KT - 4380）对假单胞菌属以及其他革兰氏阴性菌株的活性最强。
