Browsing by Author "Espinosa Bustos, Christian"

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    Design, Synthesis, Binding and Docking-Based 3D-QSAR Studies of 2-Pyridylbenzimidazoles—A New Family of High Affinity CB1 Cannabinoid Ligands
    (2013) Espinosa Bustos, Christian; Iturriaga Vásquez, Patricio; Lagos, Carlos; Mella Raipán, Jaime; Pessoa Mahana, Carlos David; Pessoa Mahana, Hernán; Recabarren Gajardo, Gonzalo Iván; Romero Parra, Javier Hernán
    A series of novel 2-pyridylbenzimidazole derivatives was rationally designed and synthesized based on our previous studies on benzimidazole 14, a CB1 agonist used as a template for optimization. In the present series, 21 compounds displayed high affinitie
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    Expanding the chemical space of aryloxy-naphthoquinones as potential anti-Chagasic agents: synthesis and trypanosomicidal activity
    (SPRINGER BIRKHAUSER, 2021) Becerra, Nohemi A.; Espinosa Bustos, Christian; Vazquez, Karina; Rivera, Gildardo; Paulino, Margot; Cantero, Jorge; Nogueda, Benjamin; Chacon Vargas, Fabiola; Castillo Velazquez, Uziel; Elizondo Rodriguez, Ana F.; Toledo, Sofia; Moreno Rodriguez, Adriana; Aranda, Mario; Salas, Cristian O.
    In continuation our effort to research the chemical space of aryloxy-naphthoquinones as potential anti-Chagas agents, we synthesized nine derivatives and these compounds were evaluated in vitro against the epimastigote and trypomastigote forms of Mexican strains of Trypanosoma cruzi (T. cruzi). Most of these derivatives are highly active against epimastigote forms (IC50 < 1.0 mu M) compared to the reference drug benznidazole (Bzn). Then these were evaluated on trypomastigotes, which is showing better potency results than Bzn for compounds 3b and 3g. In addition, the cytotoxicity of these compounds was determined on the murine macrophage cell line J774. 3b and 3i were the most selective compounds against NINOA trypomastigote and INC-5 epimastigote forms, respectively. Further these compounds also have good oral bioavailability according to theoretical predictions. Finally, we were able to determine optimal substitution patterns using pharmacophoric models. All these results are provided very useful structural information to continue our designing of naphthoquinone derivatives against T. cruzi.
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    Microwave-assisted synthesis and regioisomeric structural elucidation of novel benzimidazo[1,2d][1,4]benzodiazepinone derivatives
    (ARKAT USA INC, 2009) Pessoa Mahana, David; Espinosa Bustos, Christian; Mella Raipan, Jaime; Canales Pacheco, Jorge; Pessoa Mahana, Hernan
    The synthesis of 5H-benzimidazo [1,2-d] [1,4] benzodiazepin -6(7H)-ones 3a-e from readily available 2-(2-aminophenyl)-1H-benzo[d]imidazole derivatives 2a-e and 2-bromoacetyl bromide under microwave conditions is described. Unambiguous structural elucidation of the obtained regioisomers was finally established by means of 2D-NOESY experiment.