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hemoglobin degrading protease

NOT Open Access | Inhibition of Hemoglobin Degrading Protease Falcipain-2 as a Mechanism for Anti-Malarial Activity of Triazole-Amino Acid Hybrids

February 22, 2020 - 17:00 -- NOT Open Access
Author(s): 
Vigyasa Singh, Rahul Singh Hada, Amaduddin, Babita Aneja, Mohammad Abid, Kailash C. Pande, Shailja Singh
Reference: 
Current Topics in Medicinal Chemistry, 11/02/20

Novel drug development against malaria parasite over the old conventional anti-malarial drugs is essential due to rapid and indiscriminate use of drugs, which led to the emergence of resistant strains. In this study, previously reported triazole-amino acid hybrids (13-18) have been explored against Plasmodium falciparum as antimalarial agents. Among the six compounds, 15 and 18 exhibited antimalarial activity against P. falciparum with insignificant hemolytic activity and cytotoxicity towards HepG2 mammalian cells. Antimalarial half-maximal inhibitory concentration (IC50) of 15 and 18 compounds was found to be 9.26 μM and 20.62 μM, respectively.

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