Biava M, Porretta G C, Deidda D, Pompei R
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università "La Sapienza", P.le A Moro 5, 00185 Rome, Italy.
Infect Disord Drug Targets. 2006 Jun;6(2):159-72. doi: 10.2174/187152606784112173.
The resurgence of tuberculosis and the surge of multidrug-resistant clinical isolates of Mycobacterium tuberculosis have reaffirmed tuberculosis as a primary public health concern. In this review we describe some new findings on the pharmacological status of fluoroquinolones derivatives (Gatifloxacin, Moxifloxacin and Sitafloxacin), new macrolides (Clarithromycin, Azithromycin and Roxithromycin), new rifamycin derivatives (Rifapentin, Rifabutin and Rifalazil) and new oxazolidinones (Linezolid and PNU 100480). We describe also other type of agents that are being developed as antimycobacterial drugs. Some of these are under clinical investigation, while others are considered to be promising candidates for future development. Among them, nitroimidazopyrans, new ketolides, Isoxyl (ISO), pyrroles derived from BM 212, Mefloquine and Diarylquinoline R207910 are discussed. We also describe the mechanism of drug resistance in mycobacteria, as well as new potential targets.
结核病的死灰复燃以及耐多药结核分枝杆菌临床分离株的激增,再次证实结核病是主要的公共卫生问题。在本综述中,我们描述了氟喹诺酮类衍生物(加替沙星、莫西沙星和司帕沙星)、新型大环内酯类(克拉霉素、阿奇霉素和罗红霉素)、新型利福霉素衍生物(利福喷汀、利福布汀和利福拉齐)以及新型恶唑烷酮类(利奈唑胺和PNU 100480)的药理学研究新发现。我们还描述了正在研发的其他类型的抗分枝杆菌药物。其中一些正在进行临床研究,而其他一些则被认为是未来有发展前景的候选药物。本文讨论了其中的硝基咪唑并吡啶类、新型酮内酯类、异噁唑(ISO)、源自BM 212的吡咯类、甲氟喹和二芳基喹啉R207910。我们还描述了分枝杆菌的耐药机制以及新的潜在靶点。