Synthesis and Biological Evaluation of Arylthiourea Derivatives with Antitubercular Activity
作者:Rusong Luo、Tuomo Laitinen、Liyan Teng、Tapio Nevalainen、Maija Lahtela-Kakkonen、Baofu Zheng、Honghai Wang、Antti Poso、Xuelian Zhang
DOI:10.2174/1570180811310070012
日期:2013.6.1
Tuberculosis (TB) is a contagious disease caused by Mycobacterium tuberculosis (M. tuberculosis), and remains
one of the most life-threatening plagues for public health in the world. The emergence of drug resistant strains of
TB and co-infection with HIV has further complicated TB treatment. Here, the synthesis and characterizaton of a series of
compounds were described, and these were followed by evaluating for their antibacterial activity against M. tuberculosis.
Several novel arylthiourea derivatives exhibited excellent activity (lowest MIC=0.09 μg/ml) against M. tuberculosis including
drug resistant strains of M. tuberculosis. The results suggest that these compounds are promising candidates for
new anti-TB agent development.
结核病(TB)是一种由结核分枝杆菌(M. tuberculosis)引起的传染性疾病,仍然是全球公共卫生的最致命威胁之一。耐药TB菌株的出现以及与HIV的共同感染进一步复杂化了结核病的治疗。本文描述了一系列化合物的合成与表征,随后对其抗菌活性进行了评估,特别是针对结核分枝杆菌。几种新型芳基硫脲衍生物显示出卓越的活性(最低MIC=0.09 μg/ml),能有效对抗包括耐药菌株在内的结核分枝杆菌。这些结果表明,这些化合物是有希望的新型抗结核药物开发候选者。