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

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

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Abstract

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.

Item Type: Article
Subjects: R Medicine > RS Pharmacy and materia medica > RS1-441 Pharmacy and materia medica
Divisions: Pusat Pengajian Sains Farmasi (School of Pharmacy) > Thesis
Pusat Pengajian Sains Kimia (School of Chemistry) > Article
Depositing User: Mr Noorazilan Noordin
Date Deposited: 20 Sep 2017 08:41
Last Modified: 20 Sep 2017 08:41
URI: http://eprints.usm.my/id/eprint/36660

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