Click Inspired Synthesis of Novel Cinchonidine Glycoconjugates as Promising Plasmepsin Inhibitors

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,...

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Bibliographic Details
Published in:Scientific reports 2020-02, Vol.10 (1), p.3586, Article 3586
Main Authors: Mishra, Nidhi, Agrahari, Anand K., Bose, Priyanka, Singh, Sumit K., Singh, Anoop S., Tiwari, Vinod K.
Format: Article
Language:English
Subjects:
140/131
639/638/309/2132/605
639/638/403/931
Alkynes
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Aspartic Acid Endopeptidases - antagonists & inhibitors
Aspartic Acid Endopeptidases - chemistry
Catalysis
Cinchona Alkaloids - chemical synthesis
Cinchona Alkaloids - chemistry
Cinchona Alkaloids - pharmacology
Click Chemistry
Copper - chemistry
Drug Design
Drug resistance
Erythrocytes
Glycoconjugates
Humanities and Social Sciences
Humans
Malaria
Malaria, Falciparum - parasitology
Molecular Docking Simulation
Molecular Structure
multidisciplinary
Parasites
Plasmodium falciparum - drug effects
Plasmodium falciparum - enzymology
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Protozoan Proteins - antagonists & inhibitors
Protozoan Proteins - chemistry
Science
Science (multidisciplinary)
Triazoles - chemistry
Vector-borne diseases
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Summary: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.
ISSN:2045-2322
2045-2322
DOI:10.1038/s41598-020-59477-3