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Synthesis, X-Ray diffraction, Trypanocidal activity and Molecular Studies of Benzoyl Phthalimides and Isoquinolones

Author

Listed:
  • Paola L Ramírez-Hernandez
  • Erick Suárez-Contreras

    (Unidad Profesional Interdisciplinaria de Biotecnología, IPN, México)

  • Benjamin Nogueda-Torres
  • Marco A. Leyva-Ramírez
  • Efren V García-Baez

    (Escuela Nacional de Ciencia Biológicas, Carpio y Plan de Ayala Colonia Santo Tomás, México)

  • Marco Brito-Arias

    (Av.Instituto Politécnico Nacional 2508, San Pedro Zacatenco, México)

Abstract

α-Phthalimide acetophenones 1a-b, 3-benzoyl isoquinolones 2a-b were synthesized by following two pathways and evaluated as trypanosoal inhibitors in vitro, showing weak activity for 1a-b and 2a, and significant for 2b as compared with the reference drugs benznidazol. Also docking studies were carried out to determine the binding mode, the scoring functions and the interactions with the residues at the active site of the cruzain target enzyme.

Suggested Citation

  • Paola L Ramírez-Hernandez & Erick Suárez-Contreras & Benjamin Nogueda-Torres & Marco A. Leyva-Ramírez & Efren V García-Baez & Marco Brito-Arias, 2017. "Synthesis, X-Ray diffraction, Trypanocidal activity and Molecular Studies of Benzoyl Phthalimides and Isoquinolones," Organic & Medicinal Chemistry International Journal, Juniper Publishers Inc., vol. 3(2), pages 46-51, August.
    • Handle: RePEc:adp:jomcij:v:3:y:2017:i:2:p:46-51
    DOI: 10.19080/OMCIJ.2017.03.555608
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