Title of article :
Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′- Indolines as New Urease Inhibitors
Author/Authors :
Mohammadi Ziarani, Ghodsi Department of Chemistry - Alzahra University, Vanak Square, Tehran , Asadi, Shima Department of Chemistry - Alzahra University, Vanak Square, Tehran , Badiei, Alireza School of Chemistry - College of Science - University of Tehran, Tehran , Sharifi, Amirhossein Drug Design and Development Research Centre and Department of Medicinal Chemistry - Faculty of Pharmacy, TehranUniversity of Medical Sciences, Tehran , Amanlou, Massoud Drug Design and Development Research Centre and Department of Medicinal Chemistry - Faculty of Pharmacy, TehranUniversity of Medical Sciences, Tehran
Abstract :
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 IC50 =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 IC50 values of 4.35, 5.557, 7.44, 2.81 and
14.46 μM, respectively (IC50 of hydroxyurea = 100 μM).
Keywords :
Urease inhibitor , Spiro indenopyridopyrimidine , Multicomponent reaction (MCR) , Autodock , Biacidic nano catalyst
Journal title :
Astroparticle Physics