3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors
Acta Pharmaceutica Sinica B
;
(6): 479-484, 2017.
Article
in English
| WPRIM
| ID: wpr-256732
ABSTRACT
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-were synthesized and screenedagainst DENV2 NS2B/NS3 protease to elucidate their binding mechanism and orientation around the active sites. Results were validated through anDENV2 NS2B/NS3 protease assay using a fluorogenic Boc-Gly-Arg-Arg-AMC substrate. Nitro derivatives of 3,5-bis(arylidene)-4-piperidones (and) emerged as promising lead molecules for novel protease inhibitors with an ICof 15.22 and 16.23 µmol/L, respectively, compared to the standard, panduratin A, having ICof 57.28 µmol/L.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
English
Journal:
Acta Pharmaceutica Sinica B
Year:
2017
Type:
Article
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