Mechanism-Based Design, Synthesis, and in vitro Antimalarial Testing of New 4-Methylated Trioxanes Structurally Related to Artemisinin: The Importance of a Carbon-Centered Radical for Antimalarial Activity

1994 ◽  
Vol 37 (9) ◽  
pp. 1256-1258 ◽  
Author(s):  
Gary H. Posner ◽  
Chang Ho Oh ◽  
Dasong Wang ◽  
Lucia Gerena ◽  
Wilbur K. Milhous ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis ◽  
Carbon Centered Radical

scholarly journals Synthetic spirocyclic endoperoxides: new antimalarial scaffolds

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 357-362 ◽  
Author(s):  
Margherita Brindisi ◽  
Sandra Gemma ◽  
Sanil Kunjir ◽  
Luisa Di Cerbo ◽  
Simone Brogi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antimalarial Activity ◽  
Design Synthesis ◽  
Docking Calculation

Design, synthesis and molecular docking calculation studies led to the identification of novel spirocyclic peroxides with in vitro and in vivo antimalarial activity.

Design, synthesis and in vitro antimalarial activity of spiroperoxides

Tetrahedron ◽  
2006 ◽  
Vol 62 (33) ◽  
pp. 7699-7711 ◽  
Author(s):  
Hong-Xia Jin ◽  
Qi Zhang ◽  
Hye-Sook Kim ◽  
Yusuke Wataya ◽  
He-Hua Liu ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis

Design, Synthesis and in vitro Antimalarial Activity of an Acylhydrazone Library.

ChemInform ◽  
2006 ◽  
Vol 37 (13) ◽  
Author(s):  
Patricia Melnyk ◽  
Virginie Leroux ◽  
Christian Sergheraert ◽  
Philippe Grellier
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis

Thiosemicarbazone derivatives: Design, synthesis and in vitro antimalarial activity studies

2019 ◽  
Vol 137 ◽  
pp. 104986 ◽  
Author(s):  
Ramkishore Matsa ◽  
Parameshwar Makam ◽  
Meenakshi Kaushik ◽  
S.L. Hoti ◽  
Tharanikkarasu Kannan
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis

ChemInform Abstract: 4-Aminoquinoline-1,3,5-triazine: Design, Synthesis, in vitro Antimalarial Activity and Docking Studies.

ChemInform ◽  
2014 ◽  
Vol 45 (4) ◽  
pp. no-no
Author(s):  
Hans Raj Bhat ◽  
Udaya Pratap Singh ◽  
Prashant Gahtori ◽  
Surajit Kumar Ghosh ◽  
Kabita Gogoi ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Docking Studies ◽  
Design Synthesis

4-Aminoquinoline-1,3,5-triazine: Design, synthesis, in vitro antimalarial activity and docking studies

2013 ◽  
Vol 37 (9) ◽  
pp. 2654 ◽  
Author(s):  
Hans Raj Bhat ◽  
Udaya Pratap Singh ◽  
Prashant Gahtori ◽  
Surajit Kumar Ghosh ◽  
Kabita Gogoi ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Docking Studies ◽  
Design Synthesis

Design, synthesis and in vitro antimalarial activity of an acylhydrazone library

2006 ◽  
Vol 16 (1) ◽  
pp. 31-35 ◽  
Author(s):  
Patricia Melnyk ◽  
Virginie Leroux ◽  
Christian Sergheraert ◽  
Philippe Grellier
Keyword(s):  
Antimalarial Activity ◽  
Design Synthesis

Design, Synthesis, Antimalarial Activity and Docking Study of 7-Chloro-4- (2-(substituted benzylidene)hydrazineyl)quinolines

2020 ◽  
Vol 16 (7) ◽  
pp. 928-937 ◽  
Author(s):  
Jahnabi Kalita ◽  
Dipak Chetia ◽  
Mithun Rudrapal
Keyword(s):  
Antimalarial Drug ◽  
Disease Burden ◽  
Antimalarial Activity ◽  
Docking Study ◽  
Molecular Scaffold ◽  
Design Synthesis ◽  
Antimalarial Agents ◽  
Drug Molecules ◽  
Resistant Strains

Background: Malaria is a growing infectious disease burden due to the increasing emergence of resistant strains of Plasmodium falciparum. Because of the limited therapeutic efficacy of available antimalarial drugs, the development of potent antimalarial drug agents is therefore an urgent requirement to fight against resistant malaria. Objective: The objective of this work was to develop novel quinoline-baed antimalarial agents that would be active against resistant P. falciparum malaria. Methods: Some 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines were synthesized for the evaluation of their potential as possible antimalarial agents, particularly against resistant malaria. The antimalarial activity of synthesized compounds was evaluated in vitro against bloodstage parasites of P. falciparum. Further, molecular docking and drug-likeness including ADMET (Absorption, Distribution, Metabolism, Elimination and Toxicity) studies were also carried out using in silico tools. Results: Results reveal the in vitro antimalarial activity of synthesized 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines against P. falciparum. The docking study investigates the antimalarial effectiveness of synthesized quinolines as novel plasmepsin 2 inhibitors. Drug-likeness prediction exhibits acceptable drug-likeness and ADMET properties. Conclusion: Based upon our findings, it is concluded that the molecular scaffold of 7-chloro-4-(2- (substituted benzylidene)hydrazineyl)quinolines may be used as a lead structure for further modifications in the search of more potent antimalarial drug molecules.

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