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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5242352/ https://www.ncbi.nlm.nih.gov/pubmed/28228804 |
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author | Mohammadi Ziarani, Ghodsi Asadi, Shima Badiei, Alireza Sharifi, Amirhossein Amanlou, Massoud |
author_facet | Mohammadi Ziarani, Ghodsi Asadi, Shima Badiei, Alireza Sharifi, Amirhossein Amanlou, Massoud |
author_sort | Mohammadi Ziarani, Ghodsi |
collection | PubMed |
description | 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). |
format | Online Article Text |
id | pubmed-5242352 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-52423522017-02-22 Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors Mohammadi Ziarani, Ghodsi Asadi, Shima Badiei, Alireza Sharifi, Amirhossein Amanlou, Massoud Iran J Pharm Res Original Article 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). Shaheed Beheshti University of Medical Sciences 2016 /pmc/articles/PMC5242352/ /pubmed/28228804 Text en © 2016 by School of Pharmacy Shaheed Beheshti University of Medical Sciences and Health Services |
spellingShingle | Original Article Mohammadi Ziarani, Ghodsi Asadi, Shima Badiei, Alireza Sharifi, Amirhossein Amanlou, Massoud Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title | Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title_full | Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title_fullStr | Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title_full_unstemmed | Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title_short | Synthesis of Some Spiro Indeno[1,2-b]pyrido[2,3-d]Pyrimidine-5,3′-Indolines as New Urease Inhibitors |
title_sort | synthesis of some spiro indeno[1,2-b]pyrido[2,3-d]pyrimidine-5,3′-indolines as new urease inhibitors |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5242352/ https://www.ncbi.nlm.nih.gov/pubmed/28228804 |
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