| ชื่อเรื่อง | : | 3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors |
| นักวิจัย | : | Osman, Hasnah , Idris, Nor Hashima , Kamarulzaman, Ezatul Ezleen , A. Wahab, Habibah , Hassan, Mohd. Zaheen |
| คำค้น | : | QD1-999 Chemistry , RS1-441 Pharmacy and materia medica |
| หน่วยงาน | : | Universiti Sains Malaysia, Malaysia |
| ผู้ร่วมงาน | : | - |
| ปีพิมพ์ | : | 2560 |
| อ้างอิง | : | 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 |
| ที่มา | : | - |
| ความเชี่ยวชาญ | : | - |
| ความสัมพันธ์ | : | http://dx.doi.org/10.1016/j.apsb.2017.04.009 , http://eprints.usm.my/37959/ |
| ขอบเขตของเนื้อหา | : | - |
| บทคัดย่อ/คำอธิบาย | : | 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. |
| บรรณานุกรม | : |
Osman, Hasnah , Idris, Nor Hashima , Kamarulzaman, Ezatul Ezleen , A. Wahab, Habibah , Hassan, Mohd. Zaheen . (2560). 3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors.
กรุงเทพมหานคร : Universiti Sains Malaysia, Malaysia. Osman, Hasnah , Idris, Nor Hashima , Kamarulzaman, Ezatul Ezleen , A. Wahab, Habibah , Hassan, Mohd. Zaheen . 2560. "3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors".
กรุงเทพมหานคร : Universiti Sains Malaysia, Malaysia. Osman, Hasnah , Idris, Nor Hashima , Kamarulzaman, Ezatul Ezleen , A. Wahab, Habibah , Hassan, Mohd. Zaheen . "3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors."
กรุงเทพมหานคร : Universiti Sains Malaysia, Malaysia, 2560. Print. Osman, Hasnah , Idris, Nor Hashima , Kamarulzaman, Ezatul Ezleen , A. Wahab, Habibah , Hassan, Mohd. Zaheen . 3,5-Bis(arylidene)-4-piperidones as potential dengue protease inhibitors. กรุงเทพมหานคร : Universiti Sains Malaysia, Malaysia; 2560.
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