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1篇 您的检索式:作者名="Nor Hashima Idris"
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13,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors显示文摘Dengue is a severe mosquito-borne viral infection causing half a million deaths annually.Dengue virus NS2B/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-bis(arylidene)-4-piperidones(4e and 4j) emerged as promising lead molecules for novel protease inhibitors with an IC50 of 15.22 and16.23 mmol/L, respectively, compared to the standard, panduratin A, having IC50 of 57.28 mmol/L.Hasnah Osman Nor Hashima Idris Ezatul Ezleen Kamarulzaman Habibah A.Wahab Mohd.Zaheen Hassan 2017Acta Pharmaceutica Sinica B2017,7,4:0
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