Preparation and antimalarial activities of ⟪4 trioxaquines⟫, new modular molecules with a trioxane skeleton linked to a 4-aminoquinoline

被引:0
|
作者
Dechy-Cabaret, O
Benoit-Vical, F
Robert, A
Meunier, B
机构
[1] CNRS, Chim Coordinat Lab, F-31077 Toulouse 4, France
[2] INSERM, F-75654 Paris 13, France
来源
ACTUALITE CHIMIQUE | 2001年 / 09期
关键词
aminoquinoline; drug research; malaria; peroxide; trioxaquine;
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Trioxaquines are new antimalarial drugs which combine two active fragments (an aminoquinoline and a trioxane) with independant modes of action covalently linked within a single molecule. This strategy, which can be characterized as a much less than covalent bitherapy much greater than allowed us to obtain modular molecules with high antimalarial activity in vitro either on chloroquine sensitive or on chloroquine resistant Plasmodium falciparum strains.
引用
收藏
页码:9 / 11
页数:3
相关论文
共 50 条
  • [41] Examination of novel 4-aminoquinoline derivatives designed and synthesized by a hybrid pharmacophore approach to enhance their anticancer activities
    V. Raja Solomon
    Sheetal Pundir
    Hoyun Lee
    Scientific Reports, 9
  • [42] Application of multicomponent reactions to antimalarial drug discovery.: Part 2:: New antiplasmodial and antitrypanosomal 4-aminoquinoline γ- and δ-lactams via a 'catch and release' protocol
    Musonda, Chitalu C.
    Gut, Jiri
    Rosenthal, Philip J.
    Yardley, Vanessa
    De Souza, Renata C. Carvalho
    Chibale, Kelly
    BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (16) : 5605 - 5615
  • [43] A new route for the synthesis of highly substituted 4-aminoquinoline drug like molecules via aza hetero-Diels-Alder reaction
    Vidyacharan, Shinde
    Sagar, A.
    Sharada, Duddu S.
    ORGANIC & BIOMOLECULAR CHEMISTRY, 2015, 13 (28) : 7614 - 7618
  • [44] Synthesis and In Vitro Antimalarial Activity Evaluation of Some New 1,2-Diaminopropane Side-Chain-Modified 4-Aminoquinoline Mannich Bases
    Singh, Bhupendra
    Chetia, Dipak
    Kumawat, Mukesh Kumar
    PHARMACEUTICAL CHEMISTRY JOURNAL, 2021, 55 (07) : 724 - 731
  • [45] Synthesis and In Vitro Antimalarial Activity Evaluation of Some New 1,2-Diaminopropane Side-Chain-Modified 4-Aminoquinoline Mannich Bases
    Bhupendra Singh
    Dipak Chetia
    Mukesh Kumar Kumawat
    Pharmaceutical Chemistry Journal, 2021, 55 : 724 - 731
  • [46] A novel 4-aminoquinoline chemotype with multistage antimalarial activity and lack of cross-resistance with PfCRT and PfMDR1 mutants
    Ferreira, Leticia Tiburcio
    Cassiano, Gustavo Capatti
    Alvarez, Luis Carlos Salazar
    Okombo, John
    Calit, Juliana
    Fontinha, Diana
    Gil-Iturbe, Eva
    Coyle, Rachael
    Andrade, Carolina Horta
    Sunnerhagen, Per
    Bargieri, Daniel Youssef
    Prudencio, Miguel
    Quick, Matthias
    Cravo, Pedro V.
    Lee, Marcus C. S.
    Fidock, David A.
    Costa, Fabio Trindade Maranhao
    PLOS PATHOGENS, 2024, 20 (10)
  • [47] Design, synthesis and anti-plasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives
    Chiyanzu, I
    Clarkson, C
    Smith, PJ
    Lehman, J
    Gut, J
    Rosenthal, PJ
    Chibale, K
    BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (09) : 3249 - 3261
  • [48] Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts
    Musonda, CC
    Taylor, D
    Lehman, J
    Gut, J
    Rosenthal, PJ
    Chibale, K
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (15) : 3901 - 3905
  • [49] IN VITRO AND IN VIVO EVALUATION AND EARLY TRANSITIONING STUDIES OF NOVEL QUINOLIZIDINYL-AND QUINOLIZIDINYLALKYL- DERIVATIVES OF 4-AMINOQUINOLINE WITH POTENT ANTIMALARIAL ACTIVITY
    Taramelli, Donatella
    Basilico, Nicoletta
    Casagrande, Manolo
    Corbett, Yolanda
    Parapini, Silvia
    Romeo, Sergio
    Rusconi, Carla
    Tosi, Alessia
    van den Bogaart, Erika
    Vivas, Livia
    Jabes, Daniela
    Sparatore, Anna
    AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 2008, 79 (06): : 286 - 287
  • [50] Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity
    Thelingwani, Roslyn
    Bonn, Britta
    Chibale, Kelly
    Masimirembwa, Collen
    EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY, 2014, 10 (10) : 1313 - 1324