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3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors

Dengue isaseveremosquito-borneviralinfectioncausinghalfamilliondeathsannually. Dengue virusNS2B/NS3proteaseisavalidatedtargetforanti-denguedrugdesign.Aseriesofhitherto unreported 3,5-bis(arylidene)-4-piperidonesanalogues 4a–4j were synthesizedandscreened in silico against DENV2NS2B/NS3proteasetoe...

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Main Authors: Osman, Hasnah, Idris, Nor Hashima, Kamarulzaman, Ezatul Ezleen, A.Wahab, Habibah, Hassan, Mohd. Zaheen
Format: Article
Published: Elsevier 2017
Subjects:
RS1-441 Pharmacy and materia medica
Online Access:http://eprints.usm.my/36660/
http://dx.doi.org/10.1016/j.apsb.2017.04.009
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spelling my.usm.eprints.36660 http://eprints.usm.my/36660/ 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors Osman, Hasnah Idris, Nor Hashima Kamarulzaman, Ezatul Ezleen A.Wahab, Habibah Hassan, Mohd. Zaheen RS1-441 Pharmacy and materia medica Dengue isaseveremosquito-borneviralinfectioncausinghalfamilliondeathsannually. Dengue virusNS2B/NS3proteaseisavalidatedtargetforanti-denguedrugdesign.Aseriesofhitherto unreported 3,5-bis(arylidene)-4-piperidonesanalogues 4a–4j were synthesizedandscreened in silico against DENV2NS2B/NS3proteasetoelucidatetheirbindingmechanismandorientationaroundthe active sites.Resultswerevalidatedthroughan in vitro DENV2 NS2B/NS3proteaseassayusinga fluorogenic Boc-Gly-Arg-Arg-AMCsubstrate.Nitroderivativesof3,5-bis(arylidene)-4-piperidones(4e and 4j) emergedaspromisingleadmoleculesfornovelproteaseinhibitorswithanIC50 of 15.22and 16.23 mmol/L, respectively,comparedtothestandard,panduratinA,havingIC50 of 57.28 mmol/L. Elsevier 2017 Article PeerReviewed Osman, Hasnah and Idris, Nor Hashima and Kamarulzaman, Ezatul Ezleen and A.Wahab, Habibah and Hassan, Mohd. Zaheen (2017) 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors. Acta Pharmaceutica Sinica B, 7 (4). pp. 479-484. ISSN 2211-3835 http://dx.doi.org/10.1016/j.apsb.2017.04.009
institution Universiti Sains Malaysia
building Hamzah Sendut Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Sains Malaysia
content_source USM Institutional Repository
url_provider http://eprints.usm.my/
topic RS1-441 Pharmacy and materia medica
spellingShingle RS1-441 Pharmacy and materia medica
Osman, Hasnah
Idris, Nor Hashima
Kamarulzaman, Ezatul Ezleen
A.Wahab, Habibah
Hassan, Mohd. Zaheen
3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
description Dengue isaseveremosquito-borneviralinfectioncausinghalfamilliondeathsannually. Dengue virusNS2B/NS3proteaseisavalidatedtargetforanti-denguedrugdesign.Aseriesofhitherto unreported 3,5-bis(arylidene)-4-piperidonesanalogues 4a–4j were synthesizedandscreened in silico against DENV2NS2B/NS3proteasetoelucidatetheirbindingmechanismandorientationaroundthe active sites.Resultswerevalidatedthroughan in vitro DENV2 NS2B/NS3proteaseassayusinga fluorogenic Boc-Gly-Arg-Arg-AMCsubstrate.Nitroderivativesof3,5-bis(arylidene)-4-piperidones(4e and 4j) emergedaspromisingleadmoleculesfornovelproteaseinhibitorswithanIC50 of 15.22and 16.23 mmol/L, respectively,comparedtothestandard,panduratinA,havingIC50 of 57.28 mmol/L.
format Article
author Osman, Hasnah
Idris, Nor Hashima
Kamarulzaman, Ezatul Ezleen
A.Wahab, Habibah
Hassan, Mohd. Zaheen
author_facet Osman, Hasnah
Idris, Nor Hashima
Kamarulzaman, Ezatul Ezleen
A.Wahab, Habibah
Hassan, Mohd. Zaheen
author_sort Osman, Hasnah
title 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_short 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_full 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_fullStr 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_full_unstemmed 3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_sort 3,5-bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
publisher Elsevier
publishDate 2017
url http://eprints.usm.my/36660/
http://dx.doi.org/10.1016/j.apsb.2017.04.009
_version_ 1643708847391506432
score 13.18916

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