羟基修饰与药物抗菌活性研究进展

Progress in Hydroxyl Structure-activity Relationship Study of Antibiotics

修饰羟基可提高大多数抗菌药物的药效,研究中一般对羟基进行以下4种修饰:酰化为酰胺或酯类;烷化或烷氧化;用卤素取代;直接将羟基去除。经这些修饰后,可起到增强抗菌活性、对抗耐药性、方便制剂的作用,但羟基的修饰并非对所有的抗菌药物都是有利的,所以在修饰羟基时应视具体情况而定。

Modify antibiotics structure in terms of increased therapeutic effectiveness, reduced activity on multi drug resistance or both. Previous hydroxyl structure-activity studies had shown that modifications of the hydroxyl structure can result not only in active agents, but more importantly, analogues with reduced activity on drug resistance. The fact that hydroxyl derivatives showed higher potency than pre-antibiotics, prompted us to explore novel analogues with altered substitution patterns on the hydroxyl. In this paper it is described that hydroxyl was either removed or replaced with acyl or alkyl or halobiont groups.