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Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors

New series of spiro indeno[1,2-b]pyrido[2,3-d]pyrimidine-5,3′-indolines as new urease inhibitors were synthesized by the catalytic procedure in high yield and short reaction time. In this method, biacidic carbon was prepared as a novel heterogeneous acid and was subsequently used as an efficient cat...

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Detalles Bibliográficos
Autores principales: Mohammadi Ziarani, Ghodsi, Asadi, Shima, Badiei, Alireza, Sharifi, Amirhossein, Amanlou, Massoud
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5242352/
https://www.ncbi.nlm.nih.gov/pubmed/28228804
Descripción
Sumario:New series of spiro indeno[1,2-b]pyrido[2,3-d]pyrimidine-5,3′-indolines as new urease inhibitors were synthesized by the catalytic procedure in high yield and short reaction time. In this method, biacidic carbon was prepared as a novel heterogeneous acid and was subsequently used as an efficient catalyst. The inhibitory activities of synthesized compounds were tested against Jack bean urease using Berthelot colorimetric assay and docking simulation using AutoDock 4.2. The compound 4a with IC(50) =1.94 µM has the most inhibitor activity in this study. Other derivatives such as 4b, 4d, 4e and 7a were found to be more potent urease inhibitors than the standard inhibitor hydroxyurea, yielding IC(50) values of 4.35, 5.557, 7.44, 2.81 and 14.46 μM, respectively (IC(50) of hydroxyurea = 100 μM).