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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

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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Carboxymethyl glycoside lactone(CMGL) synthons:Scope of the method and preliminary results on step growth polymerization of α-azide-ω-alkyne glycomonomers

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Science China Chemistry 2010年第9期53卷 1880-1887页

作者： CHAMBERT Stéphane BERNARD Julien FLEURY Etienne QUENEAU Yves INSA-Lyon Laboratoire de Chimie Organique et Bioorganique Bat.J.Verne 20 Avenue A.Einstein69621 Villeurbanne CedexFrance ICBMS Institut de Chimie et de Biochimie Moléculaires et SupramoléculairesUMR5246 CNRS université de Lyon université Lyon 1 INSA-Lyon CPE-Lyon Bat.Curien 43 Bd du 11 Novembre 1918F 69622 VilleurbanneFrance INSA-LYON IMP1ngénierie des Matériaux Polymères UMR5223 université de Lyon université Claude Bernard Lyon 1F-69621 Villeurbanne CedexFrance

Carboxymethyl glycoside lactones(CMGLs) are bicyclic synthons which open readily for accessing new types of pseudo-glycoconjugates,such as sugar-amino acid hybrids,neoglycolipids,pseudodisaccharides,and membrane imaging *** lactone opening,free OH-2 is available for further functionalization,leading to 1,2-bisfunctionalized *** strategy is illustrated herein with new polymerizable systems of the AB type bearing both azide and alkyne functions prepared from α or β gluco-CMGL *** the reaction of lactones with propargylamine,an azido group was introduced by two different sequences leading to either the 2-manno-azido or the 6-gluco-azido *** capability of these AB monomers to undergo step growth polymerization through copper(I) catalyzed alkyne-azide cycloaddition(CuAAC) and generate glycopolytriazoles was evidenced.

关键词： carbohydrates glycopolymers lactones click chemistry step growth polymerization glycoconjugates azides alkynes huisgen cycloaddition

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