...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Antimicrobial agents and chemotherapy. >Identification of (+)-erythro-mefloquine as an active enantiomer with greater efficacy than mefloquine against Mycobacterium avium infection in mice
【24h】

Identification of (+)-erythro-mefloquine as an active enantiomer with greater efficacy than mefloquine against Mycobacterium avium infection in mice

机译：鉴定（+）-赤型-甲氟喹为活性对映体，其抗甲鸟分枝杆菌感染小鼠的功效比甲氟喹更大

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Infection caused by Mycobacterium avium is common in AIDS patients who do not receive treatment with highly active antiretroviral therapy (HAART) or who develop resistance to anti-HIV therapy. Mefloquine, a racemic mixture used for malaria prophylaxis and treatment, is bactericidal against M. avium in mice. MICs of (+)-erythro-, (-)-erythro-, (+)-threo-, and (-)-threo-mefloquine were 32 μg/ml, 32 μg/ml, 64 μg/ml, and 64 μg/ml, respectively. The postantibiotic effect for (+)-erythromefloquine was 36 h (MIC) and 41 h for a concentration of 4xMIC. The mefloquine postantibiotic effect was 25 h (MIC and 4xMIC). After baseline infection was established (7 days), the (+)- and (-)-isomers of the diastereomeric threo- and erythro-α-(2-piperidyl)-2,8- bis(trifluoromethyl)-4-quinolinemethanol were individually used to orally treat C57BL/6 bg +/bg + beige mice that were infected intravenously with M. avium. Mice were also treated with commercial mefloquine and diluent as controls. After 4 weeks of treatment, the mice were harvested, and the number of bacteria in spleen and liver was determined. Mice receiving (+)- or (-)-threo-mefloquine or (-)-erythro-mefloquine had numbers of bacterial load in tissues similar to those of untreated control mice at 4 weeks. Commercial mefloquine had a bactericidal effect. However, mice given the (+)-erythro-enantiomer for 4 weeks had a significantly greater reduction of bacterial load than those given mefloquine. Thus, (+)-erythro-mefloquine is the active enantiomer of mefloquine against M. avium and perhaps other mycobacteria.
机译：鸟分枝杆菌引起的感染常见于未接受高活性抗逆转录病毒疗法（HAART）治疗或对抗HIV疗法产生抗药性的AIDS患者。甲氟喹是一种用于预防和治疗疟疾的外消旋混合物，可在小鼠中对鸟分枝杆菌杀菌。 （+）-赤型，（-）-赤型，（+）-苏式和（-）-苏式甲喹的MIC分别为32μg/ ml，32μg/ ml，64μg/ ml和64μg / ml。 （+）-erythromefloquine的后抗生素作用为36小时（MIC），浓度为4xMIC时为41小时。甲氟喹的抗生素后作用为25小时（MIC和4xMIC）。建立基线感染后（7天），非对映异构的苏-和赤-α-（2-哌啶基）-2,8-双（三氟甲基）-4-喹啉二甲醇的（+）-和（-）-异构体为单独用于口服治疗被鸟分枝杆菌静脉感染的C57BL / 6 bg + / bg +米色小鼠。还用市售甲氟喹和稀释剂作为对照处理小鼠。处理4周后，收获小鼠，并测定脾脏和肝脏中的细菌数量。在第4周，接受（+）-或（-）-苏式-甲氟喹或（-）-赤型-甲氟喹的小鼠在组织中的细菌负荷数量与未治疗的对照小鼠相似。市售甲氟喹具有杀菌作用。然而，给予（+）-赤型对映体4周的小鼠比给予甲氟喹的小鼠具有明显更大的细菌负荷降低。因此，（+）-赤型-甲氧喹是甲氧喹对鸟分枝杆菌和也许其他分枝杆菌的活性对映异构体。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号