Synthesis of novel guttiferone A derivatives: In-vitro evaluation toward Plasmodium falciparum, Trypanosoma brucei and Leishmania donovani

2013 ◽  
Vol 65 ◽  
pp. 284-294 ◽  
Author(s):  
Yann Fromentin ◽  
Nicolas Gaboriaud-Kolar ◽  
Bruno Ndjakou Lenta ◽  
Jean Duplex Wansi ◽  
Didier Buisson ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
In Vitro Evaluation

scholarly journals Antiprotozoal Activity of 1-Phenethyl-4-Aminopiperidine Derivatives

2009 ◽  
Vol 53 (9) ◽  
pp. 3815-3821 ◽  
Author(s):  
Christophe Dardonville ◽  
Cristina Fernández-Fernández ◽  
Sarah-Louise Gibbons ◽  
Nadine Jagerovic ◽  
Lidia Nieto ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Trypanosoma Cruzi ◽  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
Antiprotozoal Activity ◽  
Protozoan Parasites ◽  
Trypanosoma Brucei Rhodesiense ◽  
Reference Drug ◽  
Axenic Amastigotes

ABSTRACT A series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum). This screening identified 29 molecules selectively active against bloodstream-form T. b. rhodesiense trypomastigotes, with 50% inhibitory concentrations (IC50) ranging from 0.12 to 10 μM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 μM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 μM) but were also cytotoxic to L-6 cells, showing little selectivity for T. cruzi. None of the molecules tested showed interesting antileishmanial activity against axenic amastigotes of L. donovani. To our knowledge, this is the first report of the antitrypanosomal activity of molecules bearing the 4-aminopiperidine skeleton.

scholarly journals Synthesis of novel β-lactams and in vitro evaluation against the human malaria parasite Plasmodium falciparum

ARKIVOC ◽  
2016 ◽  
Vol 2016 (3) ◽  
pp. 214-235 ◽  
Author(s):  
Margaret A.L. Blackie ◽  
Tzu-Shean Feng ◽  
Peter J Smith ◽  
Kelly Chibale
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Human Malaria Parasite ◽  
In Vitro Evaluation ◽  
Human Malaria ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum

scholarly journals In vitro Antiprotozoal Activity of Extracts of five Turkish Lamiaceae Species

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Hasan Kirmizibekmez ◽  
Irem Atay ◽  
Marcel Kaiser ◽  
Erdem Yesilada ◽  
Deniz Tasdemir
Keyword(s):  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
Hexane Extract ◽  
Significant Activity ◽  
Trypanosoma Brucei Rhodesiense ◽  
L6 Cells ◽  
Methanolic Extracts ◽  
Aerial Parts ◽  
Organic Extracts

The in vitro antiprotozoal activities of crude methanolic extracts from the aerial parts of five Lamiaceae plants ( Salvia tomentosa, S. sclarea, S. dichroantha, Nepeta nuda subsp. nuda and Marrubium astracanicum subsp. macrodon) were evaluated against four parasitic protozoa, i.e. Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and Plasmodium falciparum. The cytotoxic potentials of the extracts on L6 cells were also evaluated. Melarsoprol, benznidazole, miltefosine, chloroquine and podophyllotoxin were used as reference drugs. All crude MeOH extracts showed antiprotozoal potential against at least three parasites, so they were dispersed in water and partitioned against n-hexane and chloroform to yield three subextracts that were screened in the same test systems. The n-hexane extract of N. nuda was the most active against T. brucei rhodesiense while the CHCl3 extracts of S. tomentosa and S. dichroantha showed significant activity against L. donovani. All organic extracts displayed in vitro antimalarial and moderate trypanocidal activities against T. cruzi with the n-hexane extract of S. sclarea being the most active against the latter. The extracts displayed low or no cytotoxicity towards mammalian L6 cells.

scholarly journals New 2-aminopyrimidine derivatives and their antitrypanosomal and antiplasmodial activities

2020 ◽  
Vol 151 (9) ◽  
pp. 1375-1385
Author(s):  
Michael Hoffelner ◽  
Usama Hassan ◽  
Werner Seebacher ◽  
Johanna Dolensky ◽  
Patrick Hochegger ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Trypanosoma Brucei ◽  
Phenyl Ring ◽  
Ring Closure ◽  
Causative Organism ◽  
Amino Group ◽  
Trypanosoma Brucei Rhodesiense ◽  
Structural Modifications ◽  
Skeletal Myoblasts

Abstract Novel 2-aminopyrimidine derivatives were prepared from acyclic starting materials, benzylidene acetones and ammonium thiocyanates, via 5 steps, including ring closure, aromatization, S-methylation, oxidation to methylsulfonyl compounds, and formation of guanidines with suitable amines. The prepared compounds differ from each other by the substitutions of their amino group and of their phenyl ring. The 2-aminopyrimidines were tested by use of microplate assays for their in vitro activities against a causative organism of sleeping sickness, Trypanosoma brucei rhodesiense, as well as against a causative organism of malaria, Plasmodium falciparum NF54. Their cytotoxic properties were determined with L-6 cells (rat skeletal myoblasts). Some of the compounds exhibited quite good antitrypanosomal activity, and others showed excellent antiplasmodial activity. The influence of the structural modifications on these activities is discussed. Graphic abstract

Screening and In Vitro Evaluation of Potential Plasmodium falciparum Leucyl Aminopeptidase Inhibitors

2016 ◽  
Vol 12 (4) ◽  
pp. 282-293 ◽  
Author(s):  
Meenakshi Chaudhary ◽  
Vineeta Singh ◽  
Anup Anvikar ◽  
Shakti Sahi
Keyword(s):  
Plasmodium Falciparum ◽  
In Vitro Evaluation ◽  
Aminopeptidase Inhibitors ◽  
Leucyl Aminopeptidase

scholarly journals In vitro evaluation of verapamil and other modulating agents in Brazilian chloroquine-resistant Plasmodium falciparum isolates

2003 ◽  
Vol 36 (1) ◽  
pp. 5-9 ◽  
Author(s):  
Carla M.S. Menezes ◽  
Karin Kirchgatter ◽  
Sílvia M. Di Santi ◽  
Carine Savalli ◽  
Fabíola G. Monteiro ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antipsychotic Drug ◽  
Antimalarial Drug ◽  
Drug Susceptibility ◽  
Multidrug Resistant ◽  
Antiplasmodial Activity ◽  
Experimental Conditions ◽  
In Vitro Evaluation ◽  
Cardiovascular Therapy

Verapamil, was assayed to record its modulating effect upon Brazilian Plasmodium falciparum isolates resistant to chloroquine. Other cardiovascular drugs known to be modulating agents in resistant malaria and/or multidrug-resistant neoplasias, including nifedipine, nitrendipine, diltiazem and propranolol, were also evaluated. Concentrations similar to those for cardiovascular therapy were used in the in vitro microtechnique for antimalarial drug susceptibility. Intrinsic antiplasmodial activity was observed from the lowest concentrations without a significant modulating action. Other reported modulating agents, such as the antipsychotic drug trifluoperazine and the antidepressants desipramine and imipramine, demonstrated similar responses under the same experimental conditions. Results suggest a much higher susceptibility of Brazilian strains, as well as an indifferent behaviour in relation to modulating agents.

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