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头孢唑南钠(cefuzonam sodium)是Lederle药厂(日本)新开发的注射用头孢菌素。它有独特的化学结构,即在头孢烯环的C-3位上有一噻二唑基硫代甲基。与第二代和第三代头孢相比,本品对需氧和厌氧性革兰氏阳性和阴性菌具有更广的抗菌谱和更强的抗菌活性。它不会产生许多甲基四唑茂硫代甲基头孢所产生的戒酒硫样(disulfriamlike)反应和低凝血酶原血症,由于上述这些优点,本品被评价为第四代头孢。合成 7-ACA(Ⅰ)与1,2,3-噻二唑-5-硫醇钠(Ⅱ)缩合,得7-氨基-3-[(1,2,3-噻二唑-5)硫代甲基]-3头孢烯-4-羧酸(Ⅲ);Ⅲ与2-(2-氯乙酰胺基噻唑基-4)-(Z)-2-甲氧基亚氨基乙酰氯盐酸盐(Ⅳ)缩合,用
Cefuzonam sodium is a new cephalosporin for injection developed by Lederle Pharmaceuticals (Japan). It has a unique chemical structure with a thiadiazolylthiomethyl group at the C-3 position of the cephem ring. Compared with the second and third generations of cephalosporins, this product has a broader antibacterial spectrum and stronger antibacterial activity against aerobic and anaerobic Gram-positive and -negative bacteria. It does not produce many methyl tetrazolothiothiomethyl cephalosporins produced by alcohol-induced disulfrimide-like reaction and low thrombin-induced hyperlipidemia, due to these advantages, the product was evaluated as the fourth generation of cephalosporins. The condensation of 7-ACA (I) with sodium 1,2,3-thiadiazole-5-thiolate (II) gives 7-amino-3 - [(1,2,3-thiadiazol-5) Methyl] -3-cephem-4-carboxylic acid (III); and III with 2- (2-chloroacetamidothiazolyl-4) - (Z) -2-methoxyiminoacetyl chloride hydrochloride (Ⅳ) condensation, use