1前期的研究发现最早发现喹诺酮酸结构及其抗菌作用的是Lesher等在合成氯喹的过程中,分离出一个副产物,具有微弱的抗菌活性,遂合成了萘啶酮酸为母核的系列化合物,对N1和C7作不同的烷基置换,对C3上的羧基进行不同的酯基取代,经体外和体内的抗菌实验,发现萘啶酸(1,nalixilic acid)具有显著杀伤革兰氏阴性菌的作用,1963年成为第一个试用喹诺酮类抗菌 1 Previous studies found that the earliest discovery of quinolone acid structure and antibacterial effect is Lesher et al in the synthesis of chloroquine process, the separation of a byproduct, with weak antibacterial activity, then the synthesis of nalidixic acid as the mother nucleus series of compounds , Different N1 and C7 alkyl substitution, the carboxyl group on C3 different ester substitution, in vitro and in vivo antimicrobial experiments and found that nalidixic acid (1, nalixilic acid) has significant killing Gram-negative bacteria In 1963, became the first quinolone antibacterial trial