Saini Deepika, Jain Sandeep, Kumar Ajay, Jain Neelam
Drug Discovery and Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar-125001.
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119.
EXCLI J. 2016 Nov 28;15:730-737. doi: 10.17179/excli2016-677. eCollection 2016.
A series of 1-(4-methylquinolin-2-yl)-4,6-diaryl-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives was synthesized by the reaction of 3-cinnamoyl-4-hydroxy-6-methyl-2-pyran-2-ones with 2-chloro-4,6-diphenylnicotinonitrile analogues in the presence of 2-hydrazino-4-methyl quinoline and ethanol. The newly synthesized compounds were characterized by IR, H NMR and mass spectral data. The synthetic series of novel quinoline-pyrazolopyridine hybrids were screened for schizont maturation assay against chloroquine sensitive 3D7 strain of , from which the most five active analogues were further evaluated for 4-day suppressive test in Swiss albino mice. Among the series, (containing 4-Cl substituent attached to both aryl ring) portrayed considerable potent antimalarial activity during as well as study.
通过3-肉桂酰基-4-羟基-6-甲基-2-吡喃-2-酮与2-氯-4,6-二苯基烟腈类似物在2-肼基-4-甲基喹啉和乙醇存在下反应，合成了一系列1-(4-甲基喹啉-2-基)-4,6-二芳基-1H-吡唑并[3,4-b]吡啶-3-胺衍生物。通过红外光谱、氢核磁共振光谱和质谱数据对新合成的化合物进行了表征。对合成的新型喹啉-吡唑并吡啶杂化物系列进行了针对氯喹敏感的3D7疟原虫株的裂殖体成熟试验筛选，从中选取最具活性的五个类似物在瑞士白化小鼠中进行了4天抑制试验。在该系列中，（两个芳环均连接有4-氯取代基）在裂殖体成熟试验以及抑制试验中均表现出相当强的抗疟活性。
