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Antimalarial activity of a novel series of artemisinin-derived 1, 2, 3-triazole dimers

Asian Pacific Journal of Tropical Medicine 2019年第5期12卷 195-203页

作者： Kabita Gogoi Gokul Baishya 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 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

Objective: To obtain suitable artimisinin-based drug candidates with high antimalarial ***: Three different reaction schemes were used to synthesize a total of 15 artemisininbased *** first synthetic scheme involved the synthesis of diazido aliphatic and aromatic compounds from commercially available dihalides and azido derivatives of *** second scheme consisted of the reaction of dibromoaliphatic compounds with sodium azide in dimethylformamide which yielded the desired ***-based compounds on treatment with sodium azide and bromotrimethylsilane in dichloromethane produced the most potent compound *** potent compound GB-1 was synthesized from artemisinin by treatment with alcohols in the presence of Aberlyst-15 in anhydrous *** 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 ***: 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 *** suppressed 59.0% parasitaemia in vivo of rodent malaria parasite Plasmodium berghei in Swiss albino model at 50 μg/kg body weight *** 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 ***: Two compounds GB-1 and GB-2 exhibited excellent in vitro antiplasmodial activity and fair in vivo antimalarial *** the two, GB-2 showed better activity which could be attributed to its strong bonding interactions with Thr255 as evidenced from the molecular docking *** helped in identifying artemisinin analogues possessing good antimalarial properties a

关键词： Antimalarial activity Artemisinin derivatives Huisgen reaction Triazole dimers Plasmodium berghei Plasmodium falciparum Molecular docking

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