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NOT Open Access | Quinoline carboxamide core moiety-based compounds inhibit P. falciparumfalcipain-2: Design, synthesis and antimalarial efficacy studies

March 2, 2021 - 15:34 -- NOT Open Access
Singh A, Kalamuddin M, Maqbool M, Mohmmed A, Malhotra P, Hoda N
Bioorg Chem. 2021 Mar;108:104514

Targeting Falcipain-2 (FP2) for the development of antimalarials is a promising and established concept in antimalarial drug discovery and development. FP2, a member of papain-family cysteine protease of the malaria parasite Plasmodium falciparum holds an important role in hemoglobin degradation pathway. A new series of quinoline carboxamide-based compounds was designed, synthesized and evaluated for antimalarial activity.

NOT Open Access | Water Bridges Play a Key Role in the Affinity and Selectivity for the Malarial Protease Falcipain-2

July 8, 2020 - 15:46 -- NOT Open Access
Hernandez Gonzalez JE, Hernández Alvarez L, Leite VBP, Pascutti PG
J Chem Inf Model. 2020 Jul 7

Falcipain-2 (FP-2) is hemoglobinase considered an attractive drug target of Plasmodium falciparum. Recently, it has been shown that peptidomimetic nitriles containing a 3-pyridine (3Pyr) moiety at P2 display high affinity and selectivity for FP-2 with respect to human cysteine cathepsins (hCats). Further characterization demonstrated that certain P3 variants of these compounds possess micromolar inhibition of parasite growth in vitro and no cytotoxicity against human cell lines.

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
Vigyasa Singh, Rahul Singh Hada, Amaduddin, Babita Aneja, Mohammad Abid, Kailash C. Pande, Shailja Singh
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.

NOT Open Access | Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

February 16, 2020 - 09:15 -- NOT Open Access
Zhu L, Shan L, Zhu J, Li L, Li S, Wang L, Wang J, Zhang S, Zhou H, Zhang W, Li H
Sci China Life Sci. 2020 Feb 9

The Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L−1.

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