利用微生物酰基转移酶立体特异性合成3-三氟甲基头孢菌素衍生物。
Stereo-specific synthesis of 3-trifluoromethylcephalosporin derivative by microbial acylase.
作者信息
Serizawa N, Nakagawa K, Kamimura S, Miyadera T, Arai M
出版信息
J Antibiot (Tokyo). 1979 Oct;32(10):1016-8. doi: 10.7164/antibiotics.32.1016.
Cephalosporin acylase (EC 3.5.1.11) obtained from Kluyvera citrophila ATCC 21285 was found to catalyze synthesis of 7-[2-(2-thienyl)acetamido]-3-trifluoromethyl-3-cephem-4-carboxylic acid from methyl thienylacetate and dl-7-amino-3-trifluoromethyl-3-cephem-4-carboxylic acid. The enzymatically-synthesized compound showed [alpha]25 D + 42.7 degrees (c 0.058, MeOH) and its biological activity was about twice as much as that of racemic 7-[2-(2-thienyl)acetamidol]-3-trifluoromethyl-3-cephem-4-carboxylic acid chemicall synthesized. As a result, N-acylation by this enzyme was demonstrated to be asymmetric synthesis.
从嗜柠檬酸克雷伯氏菌ATCC 21285中获得的头孢菌素酰基转移酶（EC 3.5.1.11）被发现可催化从噻吩基乙酸甲酯和dl-7-氨基-3-三氟甲基-3-头孢烯-4-羧酸合成7-[2-(2-噻吩基)乙酰氨基]-3-三氟甲基-3-头孢烯-4-羧酸。酶促合成的化合物在25℃时的旋光度为[α]25D + 42.7°（c 0.058，甲醇），其生物活性约为化学合成的外消旋7-[2-(2-噻吩基)乙酰氨基]-3-三氟甲基-3-头孢烯-4-羧酸的两倍。结果表明，该酶的N-酰化反应为不对称合成。
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