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/

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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
building	USM Institutional Repository
collection	Online Access
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.
first_indexed	2025-11-15T17:23:57Z
format	Article
id	usm-36660
institution	Universiti Sains Malaysia
institution_category	Local University
last_indexed	2025-11-15T17:23:57Z
publishDate	2017
publisher	Elsevier
recordtype	eprints
repository_type	Digital Repository
spelling	usm-366602017-09-20T00:41:16Z 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
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
title	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_short	3,5-Bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
title_sort	3,5-bis(arylidene)-4-piperidonesaspotential dengue proteaseinhibitors
topic	RS1-441 Pharmacy and materia medica
url	http://eprints.usm.my/36660/ http://eprints.usm.my/36660/

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

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