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In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor

A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit α-glucosidase in which compounds 28, 31 and 32 demonstrated the highes...

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Main Authors: Leong, Sze Wei, Abas, Faridah, Lam, Kok Wai, Yusoff, Khatijah
Format: Article
Language:English
Published: Elsevier 2018
Online Access:http://psasir.upm.edu.my/id/eprint/74616/1/In%20vitro%20and%20in%20silico.pdf
http://psasir.upm.edu.my/id/eprint/74616/
https://www.sciencedirect.com/science/article/abs/pii/S0960894X17312222#!
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spelling my.upm.eprints.746162020-12-10T20:51:02Z http://psasir.upm.edu.my/id/eprint/74616/ In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor Leong, Sze Wei Abas, Faridah Lam, Kok Wai Yusoff, Khatijah A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit α-glucosidase in which compounds 28, 31 and 32 demonstrated the highest activity with IC50 values ranging from 14.1 to 15.1 µM. Structure-activity comparison shows that multiple hydroxy groups are essential for α-glucosidase inhibitory activity. Meanwhile, 3,4-dihydroxyphenyl and furanyl moieties were found to be crucial in improving α-glucosidase inhibition. Molecular docking analyses further confirmed the critical role of both 3,4-dihydroxyphenyl and furanyl moieties as they bound to α-glucosidase active site in different mode. Overall result suggests that diarylpentanoids with both five membered heterocyclic ring and polyhydroxyphenyl moiety could be a new lead design in the search of novel α-glucosidase inhibitor. Elsevier 2018 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/74616/1/In%20vitro%20and%20in%20silico.pdf Leong, Sze Wei and Abas, Faridah and Lam, Kok Wai and Yusoff, Khatijah (2018) In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor. Bioorganic & Medicinal Chemistry Letters, 28 (3). 302 - 309. ISSN 0960-894X; ESSN:1464-3405 https://www.sciencedirect.com/science/article/abs/pii/S0960894X17312222#! 10.1016/j.bmcl.2017.12.048
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description A series of thirty-four diarylpentanoids derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity. Eleven compounds (19, 20, 21, 24, 27, 28, 29, 31, 32, 33 and 34) were found to significantly inhibit α-glucosidase in which compounds 28, 31 and 32 demonstrated the highest activity with IC50 values ranging from 14.1 to 15.1 µM. Structure-activity comparison shows that multiple hydroxy groups are essential for α-glucosidase inhibitory activity. Meanwhile, 3,4-dihydroxyphenyl and furanyl moieties were found to be crucial in improving α-glucosidase inhibition. Molecular docking analyses further confirmed the critical role of both 3,4-dihydroxyphenyl and furanyl moieties as they bound to α-glucosidase active site in different mode. Overall result suggests that diarylpentanoids with both five membered heterocyclic ring and polyhydroxyphenyl moiety could be a new lead design in the search of novel α-glucosidase inhibitor.
format Article
author Leong, Sze Wei
Abas, Faridah
Lam, Kok Wai
Yusoff, Khatijah
spellingShingle Leong, Sze Wei
Abas, Faridah
Lam, Kok Wai
Yusoff, Khatijah
In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
author_facet Leong, Sze Wei
Abas, Faridah
Lam, Kok Wai
Yusoff, Khatijah
author_sort Leong, Sze Wei
title In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
title_short In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
title_full In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
title_fullStr In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
title_full_unstemmed In vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
title_sort in vitro and in silico evaluations of diarylpentanoid series as a-glucosidase inhibitor
publisher Elsevier
publishDate 2018
url http://psasir.upm.edu.my/id/eprint/74616/1/In%20vitro%20and%20in%20silico.pdf
http://psasir.upm.edu.my/id/eprint/74616/
https://www.sciencedirect.com/science/article/abs/pii/S0960894X17312222#!
_version_ 1687395151703441408
score 13.211869

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