New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: Biological evaluation and structure-activity relationships

被引：47
|
作者：
Bollini, Mariela [1 ]
Jose Casal, Juan [1 ]
Alvarez, Diego E. [1 ]
Boiani, Lucia [2 ,3 ]
Gonzalez, Mercedes [2 ,3 ]
Cerecetto, Hugo [2 ,3 ]
Maria Bruno, Ana [1 ]
机构：
[1] Univ Buenos Aires, Fac Farm & Bioquim, Dept Quim Organ, RA-1113 Buenos Aires, DF, Argentina
[2] Univ Republica, Dept Quim Organ, Fac Ciencias, Montevideo, Uruguay
[3] Univ Republica, Fac Quim, Montevideo, Uruguay
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 04期
关键词：
Imidazoisoquinolinones; QSAR; anti-Trypanosoma cruzi agents; LEISHMANIA; METABOLISM; ACIDS;
D O I：
10.1016/j.bmc.2009.01.011
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of novel benzoimidazo andN-aryl-5-oxo-imidazo[1,2-b] isoquinoline-10-carbothioamides was developed. All the compounds were evaluated for their in vitro action against the epimastigote form of Trypanosoma cruzi. Four of them showed higher activity than Nifurtimox. Their unspecific cytotoxicity was evaluated using HeLa and L6 cells, being non-toxic at concentrations at least 15 and 200 times higher than that of T. cruzi IC50. To gain insight into the mechanism of action, their DNA binding properties and reactivity with glutathione were studied, and QSAR study was performed. (c) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1437 / 1444
页数：8
相关论文
共 50 条
  • [21] New Amino Naphthoquinone Derivatives as Anti-Trypanosoma cruzi Agents Targeting Trypanothione Reductase
    Espinosa-Bustos, Christian
    Ortiz Perez, Mariana
    Gonzalez-Gonzalez, Alonzo
    Zarate, Ana Maria
    Rivera, Gildardo
    Belmont-Diaz, Javier A.
    Saavedra, Emma
    Cuellar, Mauricio A.
    Vazquez, Karina
    Salas, Cristian O.
    PHARMACEUTICS, 2022, 14 (06)
  • [22] Synthesis and Anti-Trypanosoma cruzi Biological Evaluation of Novel 2-Nitropyrrole Derivatives
    Mathias, Fanny
    Kabri, Youssef
    Brun, Damien
    Primas, Nicolas
    Di Giorgio, Carole
    Vanelle, Patrice
    MOLECULES, 2022, 27 (07):
  • [23] Pyrazol(in)e derivatives of curcumin analogs as a new class of anti-Trypanosoma cruzi agents
    Matiadis, Dimitris
    Saporiti, Tatiana
    Aguilera, Elena
    Robert, Xavier
    Guillon, Christophe
    Cabrera, Nallely
    Perez-Montfort, Ruy
    Sagnou, Marina
    Alvarez, Guzman
    FUTURE MEDICINAL CHEMISTRY, 2021, 13 (08) : 701 - 714
  • [24] Synthesis, Biological Evaluation and Structure-Activity Relationships of New Quinoxaline Derivatives as Anti-Plasmodium falciparum Agents
    Gil, Ana
    Pabon, Adriana
    Galiano, Silvia
    Burguete, Asuncion
    Perez-Silanes, Silvia
    Deharo, Eric
    Monge, Antonio
    Aldana, Ignacio
    MOLECULES, 2014, 19 (02) : 2166 - 2180
  • [25] Synthesis, anti-Trypanosoma cruzi activity and quantitative structure relationships of some fluorinated thiosemicarbazones
    Santos, Jonas da Silva
    de Melos, Jorge Luiz R.
    Lima, Gerson S.
    Lyra, Jade Crespo
    Guedes, Guilherme Pereira
    Rodrigues-Santos, Claudio Eduardo
    Echevarria, Aurea
    JOURNAL OF FLUORINE CHEMISTRY, 2017, 195 : 31 - 36
  • [26] Medicinal Plants of Chile: Evaluation of their Anti-Trypanosoma cruzi Activity
    Munoz, Orlando M.
    Maya, Juan D.
    Ferreira, Jorge
    Christen, Philippe
    San Martin, Jose
    Lopez-Munoz, Rodrigo
    Morello, Antonio
    Kemmerling, Ulrike
    ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES, 2013, 68 (5-6): : 198 - 202
  • [27] Further insights into biological evaluation of new anti-Trypanosoma cruzi 5-nitroindazoles
    Fonseca-Berzal, Cristina
    Antonio Escario, Jose
    Aran, Vicente J.
    Gomez-Barrio, Alicia
    PARASITOLOGY RESEARCH, 2014, 113 (03) : 1049 - 1056
  • [28] Oxonitrogenated Derivatives of Eremophilans and Eudesmans: Antiproliferative and Anti-Trypanosoma cruzi Activity
    Beer, Maria F.
    Reta, Guillermo F.
    Puerta, Adrian
    Bivona, Augusto E.
    Sanchez Alberti, Andres
    Cerny, Natacha
    Malchiodi, Emilio L.
    Tonn, Carlos E.
    Padron, Jose M.
    Sulsen, Valeria P.
    Donadel, Osvaldo J.
    MOLECULES, 2022, 27 (10):
  • [29] Synthesis and biological evaluation of new pyrimidin-2-one and 1,2,6-thiadiazines derivatives as anti-Trypanosoma cruzi agents
    Martinez, Sheila
    Alvarez, Guzman
    Benitez, Diego
    Varela, Javier
    Rivera, Gildardo
    Di Maio, Rossana
    Cerecetto, Hugo
    Gonzalez, Mercedes
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2011, 242
  • [30] Synthesis, cytotoxicity, and anti-Trypanosoma cruzi activity of new chalcones
    Aponte, Jose C.
    Verastegui, Manuela
    Malaga, Edith
    Zimic, Mirko
    Quiliano, Miguel
    Vaisberg, Abraham J.
    Gilman, Robert H.
    Hammond, Gerald B.
    JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (19) : 6230 - 6234
12345