title: Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3'-Indolines as New Urease Inhibitors.
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 IC50values of 4.35, 5.557, 7.44, 2.81 and 14.46 μM, respectively (IC50of hydroxyurea = 100 μM).
authors.affiliation: Department of Chemistry, Alzahra University, Vanak Square, Tehran, Iran.; National Laboratory of Pharmaceutical Research, Alzahra University, Tehran, Iran .
authors.forename: Ghodsi
authors.initials: G
authors.lastname: Mohammadi Ziarani
authors.affiliation: Department of Chemistry, Alzahra University, Vanak Square, Tehran, Iran.
authors.forename: Shima
authors.initials: S
authors.lastname: Asadi
authors.affiliation: School of Chemistry, College of Science, University of Tehran, Tehran, Iran.
authors.forename: Alireza
authors.initials: A
authors.lastname: Badiei
authors.affiliation: Drug Design and Development Research Centre and Department of Medicinal Chemistry, Faculty of Pharmacy, TehranUniversity of Medical Sciences, Tehran, Iran.
authors.forename: Amirhossein
authors.initials: A
authors.lastname: Sharifi
authors.affiliation: Drug Design and Development Research Centre and Department of Medicinal Chemistry, Faculty of Pharmacy, TehranUniversity of Medical Sciences, Tehran, Iran.
authors.forename: Massoud
authors.initials: M
authors.lastname: Amanlou
keywords: Autodock; Biacidic nano catalyst; Multicomponent reaction (MCR); Spiro indenopyridopyrimidine; Urease inhibitor