喹诺酮类药物的合成

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其抗菌谱广,口服吸收好,体内分布广,血浆蛋白结合率低,血药浓度高,故至今应用较广。

基于喹诺酮类药物的这些优点,人们对喹诺酮类药物的研究逐渐加深,喹诺酮类药物的发展也逐渐历经了第一、二、三、四代。第一代喹诺酮类抗菌药化学结构特征为氮杂萘核-4-酮-3-羧酸,因疗效不佳现已少用。第二代喹诺酮类抗菌药在第7位引入哌嗪基团,其中的吡哌酸至今仍是国内主要应用品种。随着研究的加深,研究者在喹啉环的第6位导入了氟原子7位连上哌嗪基的衍生物,第三代喹诺酮类药物(又称为氟喹诺酮类药物)随之而生,该类药物的亲水性增强,蛋白结合率降低,生物利用度提高了许多,并有良好的组织渗透性;;氟喹诺酮类抗菌谱较广和抗菌活性明显增强,几乎适用于临床常见的各种细菌感染性疾病,其对葡萄球菌等革兰阳性菌也有抗菌作用,对一些革兰阴性菌的抗菌作用则进一步加强,并对革兰阳性菌、分支杆菌、军团菌、支

喹诺酮类药物的应用现状

首席医学网2010年03月08日13:12:40 Monday

作者:栗慧玲作者单位:730700甘肃会宁县中医院

【摘要】喹诺酮类药物是近年来发现的一类新型的合成抗菌药。本文首先阐述了喹诺酮类药物的发展历史,并分别以氧氟沙星、左氧氟沙星、环丙沙星、洛美沙星、格帕沙星、莫西

Article

Preparation of anti-Pefloxacin Antibody and Development of an Indirect Competitive Enzyme-Linked Immunosorbent Assay for Detection of Pefloxacin Residue in Chicken Liver

Shengxin Lu, Yulan Zhang, Jingting Liu, Chengbiao Zhao, Wei Liu, and Rimo Xi* The School of Chemistry and Chemical Engineering, Shandong University, Jinan,

Shandong 250100, People's Republic of China

J. Agric. Food Chem., 2006, 54 (19), pp 6995–7000

DOI: 10.1021/jf061309q

Publication Date (Web): August 19, 2006

Copyright ? 2006 American Chemical Society

Section:

Food and Feed Chemistry

Abstract

Pefloxacin has been increasingly used in veterinary medicine to treat microbial infections. To avoid using a labor-intensive instrumental method to detect the residue of pefloxacin in food, a simple and convenient indirect competitive enzyme-linked immunosorbent assay method has been developed in this study. The antibody generated from immunogen cationized bovine serum albumin?pefloxacin showed high sensitivity toward pefloxacin with an IC50 value of 6.7 ppb in buffer and was suitable for a screening assay to detect the residue of pefloxacin in food products. The antibody has been assessed using rapid enzyme immunoassays to exploit its specificity. The antibody prepared shows cross-reactivity with a few other (fluoro)quinolones including fleroxacin (116%), enrofloxacin (88%), and ofloxacin (10%). The assay measured drug residue in chicken liver spiked with pefloxacin with an interassay coefficient of variation of 13.6% or less and an intra-assay coefficient of variation of 10.9% or less.

The average recovery rates at 0.5, 5, 10, 50, and 100 ppb were in the range of

86?106% for interassay and in the range of 87?103% for intra-assay, respectively. Keywords: Pefloxacin; ELISA; drug residue; antibody; immunoassay; cross-reactivity

[1]王洪权,郭惠元. 喹诺酮研究新进展[J]. 国外医药目的研究多重耐药鲍曼不动杆菌

(MDR-ABA)gyrA基因突变与环丙沙星耐药关系。方法以鲍曼不动杆菌gyrA基因序列为靶序列,用PCR+DNA测序等方法对62株临床分离株gyrA基因突变进行对比研究。结果在53株耐环丙沙星MDR-ABA菌中,有52株gyrA基因的83位表现出突变,其突变方式全为TCA→TTA,导致氨基酸丝氨酸→亮氨酸;8株环丙沙星敏感和1株环丙沙星中介的MDR-ABA菌gyrA基因无突变。结论临床分离的MDR-ABA菌对环丙沙星耐药的分子机制主要表现为gyrA基因83位氨基酸密码子突变。

王洪权; 郭惠元;

【文献出处】国外医药.抗生素分册, World Notes on Antibiotics, 编辑部邮箱1996年05期

期刊荣誉:ASPT来源刊CJFD收录刊