State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, 1111 North Zhongshan Road, Shanghai 200437, PR China.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):986-9. doi: 10.1016/j.bmcl.2008.11.078. Epub 2008 Nov 24.
Chagas' disease, caused by Trypanosoma cruzi(T. cruzi), is one of the most serious parasitic diseases in Latin America. The currently available chemotherapy, based on nifurtimox or benznidazole, is unsatisfactory due to the limited efficacy in the prevalent chronic stage of the disease and toxic side effects. In order to address these deficiencies, a series of quinolones based novel molecules have been synthesized and evaluated as potential antitrypanosomal agents. The most active analogue 10 inhibited T. cruzi with an IC(50) of 1.3 microg/mL. The results of this study have implications in the development of novel quinolone's antitrypanosomal agents.
恰加斯病由克氏锥虫（Trypanosoma cruzi，T. cruzi）引起，是拉丁美洲最严重的寄生虫病之一。目前的化疗药物基于硝呋莫司或苯硝唑，由于在疾病流行的慢性期疗效有限和毒性副作用，效果并不令人满意。为了解决这些缺陷，已经合成了一系列基于喹诺酮的新型分子，并将其作为潜在的抗锥虫药物进行了评估。最有效的类似物 10 对 T. cruzi 的抑制作用的 IC50 为 1.3 μg/mL。本研究结果对开发新型喹诺酮类抗锥虫药物具有重要意义。
