3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors

Osman, Hasnah and Idris, Nor Hashima and Kamarulzaman, Ezatul Ezleen and A. Wahab, Habibah and Hassan, Mohd. Zaheen (2017) 3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors. Acta Pharmaceutica Sinica B, 7 (4). pp. 479-484. ISSN 2211-3835

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Dengue is a severe mosquito-borne viral in fection causing half a million deaths annually. Dengue virusNS2B/NS3 protease is a validated target for anti-dengue drug design. A series of hitherto unreported 3,5-bis(arylidene)-4-piperidones analogues 4a–4j were synthesized and screened in silico against DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through an in vitro DENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate. Nitro derivatives of 3,5-is(arylidene)-4-piperidones(4e and 4j) merged as promising lead molecules for novel protease inhibitors with an IC50 of 15.22 and 16.23 umoI/L, respectively, compared to the standard, panduratin A, having IC50 of 57.28 umoI/L.

Item Type: Article
Subjects: Q Science > QD Chemistry > QD1-999 Chemistry
R Medicine > RS Pharmacy and materia medica > RS1-441 Pharmacy and materia medica
Divisions: Pusat Pengajian Sains Kajihayat (School of Biological Sciences) > Article
Pusat Pengajian Sains Kimia (School of Chemistry) > Article
Depositing User: Mr Noorazilan Noordin
Date Deposited: 18 Dec 2017 17:14
Last Modified: 19 Dec 2017 09:58
URI: http://eprints.usm.my/id/eprint/37959

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