scholarly journals Discovery of oxybisbenzoylamides as a new class of antimalarial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1173-1177 ◽  
Author(s):  
A. Pancotti ◽  
S. Parapini ◽  
M. Dell'Agli ◽  
L. Gambini ◽  
C. Galli ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
New Class ◽  
Antimalarial Agents ◽  
Dual Inhibitors

A new antimalarial pharmacophore has been obtained starting from previously described dual inhibitors of Plasmodium falciparum.

3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum

2021 ◽  
Vol 64 (6) ◽  
pp. 3035-3047
Author(s):  
Tanja C. Knaab ◽  
Jana Held ◽  
Bjoern B. Burckhardt ◽  
Kelly Rubiano ◽  
John Okombo ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
New Class ◽  
Orally Active

The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc1protein complex

MedChemComm ◽  
2012 ◽  
Vol 3 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Robin Cowley ◽  
Suet Leung ◽  
Nicholas Fisher ◽  
Mohammed Al-Helal ◽  
Neil G. Berry ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Agents

Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely

2017 ◽  
Vol 25 (24) ◽  
pp. 6467-6478 ◽  
Author(s):  
Wenhua Chen ◽  
Zhenghui Huang ◽  
Wanyan Wang ◽  
Fei Mao ◽  
Longfei Guan ◽  
...  
Keyword(s):  
Second Generation ◽  
Antimalarial Agents ◽  
Dual Inhibitors

Specific Inhibitors of Plasmodium falciparum Thioredoxin Reductase as Potential Antimalarial Agents.

ChemInform ◽  
2006 ◽  
Vol 37 (30) ◽  
Author(s):  
A. D. Adricopulo ◽  
M. B. Akoachere ◽  
R. Krogh ◽  
C. Nickel ◽  
M. J. McLeish ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Thioredoxin Reductase ◽  
Antimalarial Agents ◽  
Specific Inhibitors

scholarly journals Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Dina Coertzen ◽  
Janette Reader ◽  
Mariëtte van der Watt ◽  
Sindisiwe H. Nondaba ◽  
Liezl Gibhard ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Control ◽  
Malaria Parasite ◽  
Redox Homeostasis ◽  
New Drugs ◽  
Content Type ◽  
Artemisinin Derivatives ◽  
Antimalarial Agents ◽  
Redox Partner ◽  
Emergence Of Resistance

ABSTRACT The emergence of resistance toward artemisinin combination therapies (ACTs) by the malaria parasite Plasmodium falciparum has the potential to severely compromise malaria control. Therefore, the development of new artemisinins in combination with new drugs that impart activities toward both intraerythrocytic proliferative asexual and transmissible gametocyte stages, in particular, those of resistant parasites, is urgently required. We define artemisinins as oxidant drugs through their ability to oxidize reduced flavin cofactors of flavin disulfide reductases critical for maintaining redox homeostasis in the malaria parasite. Here we compare the activities of 10-amino artemisinin derivatives toward the asexual and gametocyte stages of P. falciparum parasites. Of these, artemisone and artemiside inhibited asexual and gametocyte stages, particularly stage V gametocytes, in the low-nanomolar range. Further, treatment of both early and late gametocyte stages with artemisone or artemiside combined with the pro-oxidant redox partner methylene blue displayed notable synergism. These data suggest that modulation of redox homeostasis is likely an important druggable process, particularly in gametocytes, and this finding thereby enhances the prospect of using combinations of oxidant and redox drugs for malaria control.

scholarly journals Synthesis and Antimalarial Activities of Cyclen 4-Aminoquinoline Analogs

2009 ◽  
Vol 53 (4) ◽  
pp. 1320-1324 ◽  
Author(s):  
M. O. Faruk Khan ◽  
Mark S. Levi ◽  
Babu L. Tekwani ◽  
Shabana I. Khan ◽  
Eiichi Kimura ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
High Selectivity ◽  
Antimalarial Activity ◽  
New Class ◽  
Antimalarial Agents ◽  
Sensitive Clone ◽  
Resistant Strains ◽  
Incorporation Assay

ABSTRACT In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn2+ complex]. The bisquinoline displays the most potent in vitro and in vivo antimalarial activities. It displays 50% inhibitory concentrations (IC50s) of 7.5 nM against the D6 (chloroquine-sensitive) clone of Plasmodium falciparum and 19.2 nM against the W2 (chloroquine-resistant) clone, which are comparable to those of artemisinin (10.6 and 5.0 nM, respectively) and lower than those of chloroquine (10.7 and 87.2 nM, respectively), without any evidence of cytotoxicity to mammalian cells, indicating a high selectivity index (>1,333 against D6 clone and >521 against W2 clone). Potent antimalarial activities of the bisquinoline against chloroquine- and mefloquine-resistant strains of P. falciparum were also confirmed by in vitro [3H]hypoxanthine incorporation assay. The in vivo antimalarial activity of the bisquinoline, as determined in P. berghei-infected mice, is comparable to that of chloroquine (50% effective dose, ≤1.1 mg/kg when given orally); no apparent toxicity has been observed up to the highest dose tested (3 × 30 mg/kg). The bisquinoline inhibits in vitro hemozoin (β-hematin) formation with an IC50 of 1.1 μM, which is about 10-fold more potent than chloroquine (IC50 9.5 μM). Overall, this article describes the discovery of a new class of cyclen 4-aminoquinoline analogs as potent antimalarial drugs.

Synthesis of 4-pyrido-6-aryl-2-substituted amino pyrimidines as a new class of antimalarial agents

2005 ◽  
Vol 13 (22) ◽  
pp. 6226-6232 ◽  
Author(s):  
Anu Agarwal ◽  
Kumkum Srivastava ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents

Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents

2008 ◽  
Vol 18 (24) ◽  
pp. 6530-6533 ◽  
Author(s):  
Ashok Kumar ◽  
Kumkum Srivastava ◽  
S. Raja Kumar ◽  
S.K. Puri ◽  
Prem M.S. Chauhan
Keyword(s):  
New Class ◽  
Antimalarial Agents
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