Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development of Plasmodium falciparum at the trophozoite stage.
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ABSTRACT:
SUBMITTER: Singh A
PROVIDER: S-EPMC9076119 | biostudies-literature | 2019 Nov
REPOSITORIES: biostudies-literature
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Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development of <i>Plasmodium falciparum</i> at the trophozoite stage.
Singh Anju A Kalamuddin Md M Mohmmed Asif A Malhotra Pawan P Hoda Nasimul N Hoda Nasimul N
RSC advances 20191129 67
Falcipain-2 (FP2) is a papain family cysteine protease and a key member of the hemoglobin degradation pathway, a process that is required at erythrocytic stages of <i>Plasmodium falciparum</i> to obtain amino acids. In this study, we report a set of 10 quinoline-triazole-based compounds (T1-T10) which exhibit a good binding affinity for FP2, inhibit its catalytic activity at micromolar concentrations and thereby arrest the parasite growth. Compounds T4 and T7 inhibited FP2 with IC<sub>50</sub> v ...[more]
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