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Title 

Potent inhibitors of lipoprotein-associated phospholipase A2: Benzaldehyde O-heterocycle-4-carbonyloxime

 

강력한 Lp-PLA2의 억제제인 벤즈알데히드 O-헤테로사이클-4-카르보닐옥심의 개발

Authors 

Hyung Jae JeongYong-Dae ParkHo Yong ParkI Y JeongTae Sook JeongWoo Song Lee

Publisher 

Elsevier

Issue Date 

2006

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 21, pp. 5576-5579

Keywords 

Lp-PLA2 inhibitorbenzaldehyde derivativefunctional grouplipoprotein associated phospholipase a 2 inhibitoroxime derivativephospholipasephospholipase A2 inhibitordrug inhibitiondrug potencyin vitro study

Abstract 

A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A2 (Lp-PLA2) activity were evaluated in vitro. Among them, compounds 3a, 3b, and 3m were identified to display a micromolar potency for inhibiting Lp-PLA2 in whole human plasma and isolated human LDL. Based on these results, structure-activity relationship was studied on modification of three parts of R1, R2, and R3 to identify a potent pharmacophore for Lp-PLA2. In an attempt to introduce various functional groups at R2 and R3, we discovered that replacement of less lipophilic groups led to an increase of inhibitory activity. Among the tested oxime derivatives, cyano- and morpholino-substituted analogue 4f at R2 and R3 had the highest potency with an IC50 value of 0.05 μM in whole human plasma.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2006.08.031

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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