化学 3-取代基-2-巯基咪唑化物按照从前报道过的工艺路线制备,见图1。 N-烷基甘氨酸衍生物(Ⅰ),甲酰化和环化成咪唑化合物(Ⅲ),再转化成化合物(Ⅳ)和(Ⅴ)。接着,咪唑衍生物(Ⅲ-Ⅴ)与CTX以通常的方法反应,得到化合物Ⅵ(图2)。制备的这类头孢菌素的结构见表一。抗微生物活性表二比较了这一系列化合物的体外抗菌杆菌包括缘脓杆菌显示了优越的活性。此外,试验结果也说明如下的构效关系。 1.化合物3和4由于结构上的羧基少于化合物1,导致抗菌活性相似或稍低于化合物1,对绿脓杆菌的活性明显减弱。 2.化合物2抗菌活性显示,唑咪环的活力。其中有一些化合物对不同种类的革兰氏阴性细菌显示高度活性。在与CTX和CMX比较时,对葡萄糖非发酵的革兰氏阴性 The chemical 3-substituent 2-mercaptoimidazolide was prepared according to the previously reported route, see Figure 1. The N-alkylglycine derivative (I) is formylated and cyclized to the imidazole compound (III) and then converted to the compounds (IV) and (V). Next, imidazole derivative (III-V) is reacted with CTX in the usual manner to give compound VI (Fig. 2). The structure of such cephalosporins prepared is shown in Table I. Antimicrobial Activity Table 2 compares in vitro antibacterial bacilli of this series of compounds, including Pseudomonas aeruginosa, showing superior activity. In addition, the test results also illustrate the following structure-activity relationship. 1.Compounds 3 and 4 showed less activity against Pseudomonas aeruginosa because their structural carboxyl groups were less than that of compound 1, resulting in antibacterial activity similar to or slightly lower than that of compound 1. 2. Antibacterial activity of Compound 2 showed that the activity of azole ring. Some of these compounds show high activity against different Gram-negative bacteria. Gram-negative for non-fermenting glucose when compared to CTX and CMX