Hossion Abugafar M L, Sasaki Kenji
The University of Pittsburgh, 100 Technology Drive, Pittsburgh, PA 15218, USA.
Recent Pat Antiinfect Drug Discov. 2013 Dec;8(3):198-205. doi: 10.2174/1574891x08666131210124649.
Each year in the United States, at least 2 million people become infected with bacteria that are resistant to antibiotics and at least 23,000 people die each year as a direct result of these infections (Threat report 2013). Vancomycin is an FDA approved antibiotic and is growing importance in the treatment of hospital infections, with particular emphasis on its value to fight against methicillin-resistant Staphylococcus aureus (MRSA). The increasing use of vancomycin to treat infections caused by the Gram-positive MRSA in the 1970s selected for drug-resistant enterococci, less potent than staphylococci but opportunistic in the space vacated by other bacteria and in patients with compromised immune systems. The dramatic rise of antibiotic-resistant bacteria over the past two decades has stressed the need for completely novel classes of antibacterial agents. This paper reports the recent patent review on the strategy for finding novel quercetinglycoside type antibacterial agents against vancomycin-resistant bacterial strains.
在美国,每年至少有200万人感染对抗生素耐药的细菌,每年至少有23000人直接死于这些感染(《2013年威胁报告》)。万古霉素是一种经美国食品药品监督管理局(FDA)批准的抗生素,在医院感染治疗中的重要性日益凸显,尤其强调其对抗耐甲氧西林金黄色葡萄球菌(MRSA)的价值。20世纪70年代,越来越多地使用万古霉素治疗由革兰氏阳性MRSA引起的感染,这导致了对耐药肠球菌的选择,肠球菌的效力不如葡萄球菌,但在其他细菌腾出的空间以及免疫系统受损的患者中具有机会致病性。在过去二十年中,抗生素耐药细菌的急剧增加凸显了对全新抗菌剂类别的需求。本文报道了近期关于寻找新型槲皮素糖苷类抗菌剂以对抗耐万古霉素细菌菌株策略的专利综述。