硫利达嗪衍生物对结核分枝杆菌的体外和离体活性
In vitro and ex vivo activity of thioridazine derivatives against Mycobacterium tuberculosis.
作者信息
Martins Marta, Schelz Zsuzsanna, Martins Ana, Molnar Joseph, Hajös Gyorgy, Riedl Zsuzsanna, Viveiros Miguel, Yalcin Ismail, Aki-Sener Esin, Amaral Leonard
机构信息
Unidade de Micobacterias, UPMM, Instituto de Higiene e Medicina Tropical, Universidade de Lisboa, Rua da Junqueira 96, 1394-008 Lisbon, Portugal.
出版信息
Int J Antimicrob Agents. 2007 Mar;29(3):338-40. doi: 10.1016/j.ijantimicag.2006.10.013. Epub 2007 Jan 18.
Thioridazine (TZ) has previously been shown by us to have in vitro and ex vivo activity against antibiotic-susceptible and multidrug-resistant Mycobacterium tuberculosis (MDRTB). Because current therapy of MDRTB is highly problematic even when all five 'first line of defence' drugs are employed, there is a need for effective antituberculosis drugs. New derivatives of TZ were synthesised and their in vitro activity against a reference strain of M. tuberculosis was evaluated with the aid of the BACTEC 460 system. Derivatives that presented significant activity were evaluated by ex vivo studies and were shown to enhance the killing of intracellular M. tuberculosis.
我们之前已证明硫利达嗪（TZ）对敏感及耐多药结核分枝杆菌（MDRTB）具有体外和体内活性。由于即使使用所有五种“一线防御”药物，目前MDRTB的治疗仍存在很大问题，因此需要有效的抗结核药物。合成了TZ的新衍生物，并借助BACTEC 460系统评估了它们对结核分枝杆菌参考菌株的体外活性。对具有显著活性的衍生物进行了体内研究评估，结果表明这些衍生物可增强对细胞内结核分枝杆菌的杀灭作用。
Zotero 插件