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4(S)-Lactivicin衍生物具有广谱抗菌活性,其抗菌效力已经肯定。本文报道九个4(RS)-、七个4(R)-和五个4(S)-Lactivicin衍生物对临床分离的19株革兰氏阳性和革兰氏阴性菌的体外抑菌活性测定结果,讨论了相同结构、不同构型的Lactivicin衍生物的构效关系。研究结果表明,4(R)-Lactivicin衍生物同4(S)-Lactivicin衍生物一样,具有广谱抗菌活性。且它们之间无明显的拮抗作用。而4(RS)-Lactivicin衍生物的抗菌活性基本兼具了4(R)和4(S)-Lactivicin衍生物的特点。因4(RS)-Lactivicin衍生物的合成可用价廉易得的DL—丝氨酸为原料,具有进一步开发研究的实际意义。
4 (S) -Lactivicin derivatives with broad-spectrum antibacterial activity, its antimicrobial efficacy has been confirmed. In this paper we report the in vitro antibacterial activity of nine 4 (RS) -, seven 4 (R) - and five 4 (S) -Lactivicin derivatives against 19 Gram-positive and Gram-negative bacteria isolated clinically As a result, the structure-activity relationship of Lactivicin derivatives of the same structure and different configurations was discussed. The results show that 4 (R) -Lactivicin derivatives have the same broad-spectrum antibacterial activity as 4 (S) -Lactivicin derivatives. And no obvious antagonism between them. However, the antibacterial activity of 4 (RS) -Lactivicin derivatives is characterized by both 4 (R) and 4 (S) -Lactivicin derivatives. Due to the synthesis of 4 (RS) -Lactivicin derivatives, DL-serine, which is cheap and available, can be used as raw material, which has the practical significance of further development and research.