Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors
Abstract 3-[(2-Chloroquinolin-3-yl) methylene]-5-phenylfuran-2 (3H)-one derivatives (6a–j
and 7a–j) have been synthesized and evaluated for their antimalarial activity. Three …
and 7a–j) have been synthesized and evaluated for their antimalarial activity. Three …
Structure-based approach to falcipain-2 inhibitors: synthesis and biological evaluation of 1, 6, 7-trisubstituted dihydroisoquinolines and isoquinolines
1, 4, 7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their
inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1 …
inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1 …
Quinoline carboxamide core moiety-based compounds inhibit P. falciparum falcipain-2: Design, synthesis and antimalarial efficacy studies
Abstract 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 …
established concept in antimalarial drug discovery and development. FP2, a member of …
Identification of novel class of falcipain-2 inhibitors as potential antimalarial agents
SK Chakka, M Kalamuddin, S Sundararaman… - Bioorganic & medicinal …, 2015 - Elsevier
Falcipain-2 is a papain family cysteine protease and an emerging antimalarial drug target. A
pseudo-tripeptide scaffold I was designed using in silico screening tools and the three …
pseudo-tripeptide scaffold I was designed using in silico screening tools and the three …
N 1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 …
Abstract A series of N 1-{4-[(10S)-dihydroartemisinin-10-oxyl]} phenylmethylene-N 2-(2-
methylquinoline-4-yl) hydrazine derivatives 9a–9n possessing 4-quinolylhydrazone and …
methylquinoline-4-yl) hydrazine derivatives 9a–9n possessing 4-quinolylhydrazone and …
[HTML][HTML] Design, synthesis and evaluation of 2-(4-(substituted benzoyl)-1, 4-diazepan-1-yl)-N-phenylacetamide derivatives as a new class of falcipain-2 inhibitors
The cysteine protease, falcipain-2 is an important drug target in human malaria parasite
Plasmodium falciparum. A new series of 2-(4-(substituted benzoyl)-1, 4-diazepan-1-yl)-N …
Plasmodium falciparum. A new series of 2-(4-(substituted benzoyl)-1, 4-diazepan-1-yl)-N …
Identification of novel falcipain-2 inhibitors as potential antimalarial agents through structure-based virtual screening
H Li, J Huang, L Chen, X Liu, T Chen… - Journal of medicinal …, 2009 - ACS Publications
The SPECS database was screened against falcipain-2 with two different docking methods
to identify structurally diverse nonpeptidic inhibitors. Twenty-eight nonpeptidic molecules …
to identify structurally diverse nonpeptidic inhibitors. Twenty-eight nonpeptidic molecules …
Designing novel inhibitors against falcipain-2 of Plasmodium falciparum
Coumarin containing pyrazoline derivatives have been synthesized and tested as inhibitors
of in vitro development of a chloroquine-sensitive (MRC-02) and chloroquine-resistant (RKL …
of in vitro development of a chloroquine-sensitive (MRC-02) and chloroquine-resistant (RKL …
[HTML][HTML] 2-(3,4-Dihydro-4-Oxothieno[2,3-d]pyrimidin-2-ylthio) Acetamides as a New Class of Falcipain-2 Inhibitors. 3. Design, Synthesis and Biological Evaluation
J Zhu, T Chen, J Liu, R Ma, W Lu, J Huang, H Li, J Li… - Molecules, 2009 - mdpi.com
The cysteine protease falcipain-2 (FP-2) of Plasmodium falciparum is a principal cysteine
protease and an essential hemoglobinase of erythrocytic P. falciparum trophozoites, making …
protease and an essential hemoglobinase of erythrocytic P. falciparum trophozoites, making …
De novo design of 7-aminocoumarin derivatives as novel falcipain-3 inhibitors
The availability of the crystal structure of falcipain-3, knowledge of the peptides carrying the
7-aminocoumarin moiety as falcipain-3 ligands/substrates, and a need for new antimalarial …
7-aminocoumarin moiety as falcipain-3 ligands/substrates, and a need for new antimalarial …