z-logo
open-access-imgOpen Access
Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3 -Indolines as New Urease Inhibitors
Author(s) -
Ghodsi Mohammadi Ziarani,
Shima Asadi,
Alireza Badiei,
Amirhossein Sharifi,
Massoud Amanlou
Publication year - 2016
Publication title -
iranian journal of pharmaceutical research : ijpr
Language(s) - English
DOI - 10.22037/ijpr.2016.1806
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).

The content you want is available to Zendy users.

Already have an account? Click here to sign in.
Having issues? You can contact us here
Accelerating Research

Address

John Eccles House
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom