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Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers
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作者 Kabita Gogoi Gokul Baishya +10 位作者 Biswajit Saikia Nabin Chandra Barua Chandrajit Dohutia Akalesh Kumar Verma Anil Prakash ICMR-Regional Medical Research Centre,N.E. CSIR-North-East Institute of Science and Technology Digboi College,Chemistry Department Pratiksha Institute of Pharmaceutical Scinces Cotton University,Zoology Department ICMR-National Institute for Research in Environmental Health 《Asian Pacific Journal of Tropical Medicine》 SCIE CAS 2019年第5期195-203,共9页
Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial activity.Methods: Three different reaction schemes were used to synthesize a total of 15 artemisininbased compounds.The first synt... Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial activity.Methods: Three different reaction schemes were used to synthesize a total of 15 artemisininbased compounds.The first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of artemisinin.The second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired compounds.Artemisinin-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound GB-2.Another potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous dichloromethane.The third scheme involved the Huisgen 1,3-dipolar cycloaddition between the synthesized aliphatic and aromatic diazides and two alkyne derivatives of artemisinin to obtain the desired artemisinin dimers with average yields.Results: The best in vitro antiplasmodial activity was shown by the compound GB-2 registering IC_(50) value 0.066 μg/mL against chloroquine-sensitive and 0.865 μg/mL against chloroquineresistant strains of Plasmodium falciparum.It suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight dosage.Molecular docking interactions of Plasmodium falciparum ATP6(PfATP6) protein revealed strong bonding of GB-2 with Thr255 residue which is likely to be the reason for excellent antimalarial activity of this compound.Conclusion: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial activity.Of the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking study.Study helped in identifying artemisinin analogues possessing good antimalarial properties and further research in structural alterations of the selected molecules should be carried out which may result in obtaining potent drug candidates against the malarial parasite. 展开更多
关键词 Antimalarial activity artemisinin derivatives Huisgen reaction Triazole dimers plasmodium berghei plasmodium falciparum Molecular docking
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小柴胡汤及其与青蒿素配伍用药的抗疟作用研究 被引量:2
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作者 薛宝云 叶祖光 +4 位作者 戴宝强 杨庆 肖永庆 刘晓宏 李泽琳 《中国实验方剂学杂志》 CAS 1996年第4期7-10,共4页
在伯氏鼠疟原虫感染的小鼠体内试验中研究了小柴胡汤及其与青蒿素配伍的抗疟作用。单用小柴胡汤醇提取物的抗疟作用甚微,当它和青蒿素联合用药时,二药并无抗疟增效作用,而且对伯氏鼠疟的复燃也无影响。
关键词 小柴胡汤 青蒿素 中药配伍 抗疟药
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