結核菌感染治療藥物的發展

Drug Development for the Treatment of Tuberculosis (TB) Infections

陳義龍(Yeh-Long Chen) ； 許嘉裕(Jia-Yuh Sheu) ； 曾誠齊(Cherng-Chyi Tzeng)

《化學》 61卷4期 (2003/12) Pp. 599-609

https://doi.org/10.6623/chem.2003056

摘要

長期以來對於結核菌（TB）的感染都是以streptomycin（SM），isoniazid（INH），ethambutol（EMB），pyrazinamide（PZA），與rifampicin（RFP）作為治療藥物，但仍無法十分有效的控制結核病的感染。近期結核菌感染的患者有逐漸增加的趨勢，且多屬於多重抗藥結核菌株的感染，因而使結核病的治療雪上加霜。於此我們將依（1）傳統藥物的結構修飾，（2）氟奎諾酮類（fluoroquinolone）作為有效的抗結核藥物與（3）雜環衍生物作為抗結核藥物，介紹最近的抗結核藥物的研究及發展。過去十年有為數眾多的化合物被合成並經由美國國家過敏及感染病協會（NIAID）所成立的TAACF（Tuberculosis Antimicrobial Acquisition and Coordinating Facility）進行免費抗結核菌活性篩選，其中也發現數個可繼續發展成為臨床治療結核病的新藥物。

關鍵字

抗結核藥物 ； 氟奎諾酮

並列摘要

The drugs currently used for the treatment of tuberculosis (TB) infection are streptomycin (SM), isoniazid (INH), ethambutol (EMB), pyrazinamide (PZA), and rifampicin (RFP). However, the current TB treatment regimens, although highly effective, are far from idea. Recently, the incidence of TB infection is further complicated by an increase in cases which are resistant to conventional drug therapy, especially the emergence of multi-drug resistant tuberculosis (MDR-TB). The present review focuses on the recent anti-TB drug research and development and classified as studies on (1) the structural modification of traditional anti-TB drugs; (2) the fluoroquinolone antibacterial drugs as potential chemotherapeutics for M. tuberculosis infection; and (3) heterocyclic compounds as anti-TB drugs. A large number of novel compounds have been prepared during the past decade and evaluated mostly by the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) through a research and development contract with the U.S. National Institute of Allergy and Infectious diseases. Certain novel compounds have been identified as potential anti-TB drug candidates.

並列關鍵字

anti-TB drug ； fluoroquinolone