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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-582 |
| Subject |
Novel phenylsulfonamide derivatives alleviate scopolamine-induced memory impairment via the inhibition of mPGES-1 |
| Authors |
ChangYoung Jang, YoonHyoung Moon, Da Woon Jung, Hong bin Yoon, Jae Yeol Lee*
Department of Chemistry, Kyung Hee University, Korea
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| Abstract |
Prostaglandin E2 (PGE2), has been thought to be an important mediator of inflammation in peripheral tissues, but recent studies clearly show its involvement in inflammatory brain diseases, such as ischemic stroke, Alzheimer’s disease (AD) and epilepsy. The biosynthetic pathway of PGE2 involves three sequential enzymatic actions from arachidonic acid: phospholipase A2; cyclooxygenases (COX-1 and COX-2), and prostaglandin E synthases (cPGES, mPGES-1 and mPGES-2). The successful modulation of PGE2 via the inhibition of one of three sequential enzymatic actions may therefore prevent or retard the onset of inflammatory brain diseases and thus provide a beneficial strategy for the potential brain diseases therapy. As microsomal prostaglandin E synthase (mPGES)-1 enzyme catalyzes the terminal step in the biosynthesis of COX-2-derived PGE2 from PGH2, the inhibition of mPGES-1 has been expected to suppress the PGE2 production without the side effects of classical NSAIDs and coxibs. Therefore, mPGES-1 inhibitors are expected to be injury-selective and have fewer side-effects when treating human brain diseases. Herein, we will describe the synthesis and biological evaluation of new phenylsulfonamide derivatives for the discovery of a candidate compound for the prevention against memory loss in some neurodegenerative diseases such as Alzheimer's disease. |
| E-mail |
jchy6679@naver.com |
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121st General Meeting of the KCS