Antimalarial activity of novel 4-cyano-3-methylisoquinoline inhibitors against Plasmodium falciparum: design, synthesis and biological evaluation

2016 ◽  
Vol 14 (20) ◽  
pp. 4617-4639 ◽  
Author(s):  
Melissa J. Buskes ◽  
Katherine L. Harvey ◽  
Benjamin J. Richards ◽  
Robabeh Kalhor ◽  
Rebecca M. Christoff ◽  
...  

A series of 4-cyano-3-methylisoquinolines have been shown to inhibit parasite cytokinesis and erythrocyte invasion.

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Huong Doan Thi Mai ◽  
Giang Vo Thanh ◽  
Van Hieu Tran ◽  
Van Nam Vu ◽  
Van Loi Vu ◽  
...  

A series of febrifugine analogues were designed and synthesized. Antimalarial activity evaluation of the synthetic compounds indicated that these derivatives had a strong inhibition against both chloroquine-sensitive and -resistant Plasmodium falciparum parasites. Many of them were found to be more active than febrifugine hydrochloride. The tested analogues had also a significant cytotoxicity against four cancer cell lines (KB, MCF7, LU1 and HepG2). Among the synthetic analogues, two compounds 17b and 17h displayed a moderate cytotoxicity while they exhibited a remarkable antimalarial activity.


ChemInform ◽  
2010 ◽  
Vol 27 (36) ◽  
pp. no-no
Author(s):  
L.-C. DE ALMEIDA BARBOSA ◽  
D. CUTLER ◽  
J. MANN ◽  
M. J. CRABBE ◽  
G. C. KIRBY ◽  
...  

Author(s):  
Luiz-Claudio de Almeida Barbosa ◽  
David Cutler ◽  
John Mann ◽  
M. James Crabbe ◽  
Geoffrey C. Kirby ◽  
...  

2017 ◽  
Vol 11 (1) ◽  
Author(s):  
Mallika Pathak ◽  
Himanshu Ojha ◽  
Anjani K. Tiwari ◽  
Deepti Sharma ◽  
Manisha Saini ◽  
...  

2020 ◽  
Vol 10 (1) ◽  
pp. 1846-1855

Synthesis of some novel thiazole hydrazine derivatives from thiosemicarbazones of salicylaldehyde and 5-chlorosalicylaldehyde with phenacyl bromide in ethanol under reflux condition is reported. The synthesized compounds were characterized by spectral analysis and further screened against - S. aureus, E. coli, P. aeruginosa, S. pyogenus bacteria, and against C. albicans, A. clavatus, and A. niger fungal strains. Most of the compounds were active against E. coli and C. albicans. Antimalarial screening against Plasmodium falciparum showed moderate to the good activity of the synthesized compounds but less than the standard quinine. One of the synthesized compounds (4c) exhibited promising antimalarial activity against Plasmodium falciparum with IC50 close to the standard quinine.


2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  

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