Click Inspired Synthesis of Novel Cinchonidine Glycoconjugates as Promising Plasmepsin Inhibitors

被引:13
|
作者
Mishra, Nidhi [1 ]
Agrahari, Anand K. [1 ]
Bose, Priyanka [1 ]
Singh, Sumit K. [1 ]
Singh, Anoop S. [1 ]
Tiwari, Vinod K. [1 ]
机构
[1] Banaras Hindu Univ, Inst Sci, Dept Chem, Varanasi 221005, Uttar Pradesh, India
关键词
ANTIMALARIAL-DRUG DISCOVERY; ONE-POT SYNTHESIS; PLASMODIUM-FALCIPARUM; HEMOGLOBIN DEGRADATION; SELECTIVE RECOGNITION; CHEMISTRY; SPECIFICITY; DOCKING; PATHWAY;
D O I
10.1038/s41598-020-59477-3
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Among all the malaria parasites, P. falciparum is the most predominant species which has developed drug resistance against most of the commercial anti-malarial drugs. Thus, finding a new molecule for the inhibition of enzymes of P. falciparum is the pharmacological challenge in present era. Herein, ten novel molecules have been designed with an amalgamation of cinchonidine, carbohydrate moiety and triazole ring by utilizing copper-catalyzed click reaction of cinchonidine-derived azide and clickable glycosyl alkynes. The molecular docking of developed molecules showed promising results for plasmepsin inhibition in the form of effective binding with target proteins.
引用
收藏
页数:17
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