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

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...

Full description

Saved in:
Bibliographic Details
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
Tags: Add Tag
No Tags, Be the first to tag this record!
Institution: Universiti Sains Malaysia
Description
Summary: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.

Similar Items