Faidallah Hassan M, Panda Siva S, Serrano Juan C, Girgis Adel S, Khan Khalid A, Alamry Khalid A, Therathanakorn Tanya, Meyers Marvin J, Sverdrup Francis M, Eickhoff Christopher S, Getchell Stephen G, Katritzky Alan R
Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA.
Bioorg Med Chem. 2016 Aug 15;24(16):3527-39. doi: 10.1016/j.bmc.2016.05.060. Epub 2016 May 30.
Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a-g, 10a-o, 11a-h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields. Some of the synthesized analogs (11a, 11d-h) exhibited antimalarial properties against Plasmodium falciparum strain 3D7 with potency higher than that of quinine (standard reference used) through in vitro standard procedure bio-assay. Statistically significant BMLR-QSAR model describes the bio-properties, validates the observed biological observations and identifies the most important parameters governing bio-activity.
点击化学技术通过苯并三唑介导的合成方法，以优异的产率得到了新型的1,2,3 - 三唑 - 奎宁共轭物8a - g、10a - o、11a - h和13。通过体外标准程序生物测定，一些合成类似物（11a、11d - h）对恶性疟原虫3D7株表现出抗疟特性，其效力高于奎宁（使用的标准参考物）。具有统计学意义的BMLR - QSAR模型描述了生物特性，验证了观察到的生物学现象，并确定了控制生物活性的最重要参数。
