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Title 

Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF 1 production

Authors 

B LeeJ H KwakS W HuangJ Y JangS LimYoung Shin KwakK LeeH S KimS B HanJ T HongH LeeS SongS Y SeoJ K Jung

Publisher 

Elsevier

Issue Date 

2012

Citation 

Bioorganic & Medicinal Chemistry, vol. 20, no. 9, pp. 2860-2868

Keywords 

4-O-MethylhonokiolAryl carbamateCyclooxygenase-2 (COX-2)IsoxazoleTriazole

Abstract 

A series of novel 4-O-methylhonokiol analogs were synthesized in light of revealing structure-activity relationship for inhibitory effect of COX-2 enzyme. The key strategy of the molecular design was oriented towards modification of the potential metabolic soft spots (e.g., phenol and olefin) or by altering the polar surface area via incorporating heterocycles such as isoxazole and triazole. Most of all exhibited the inhibitory effects on COX-2 and PGF 1 production but not macrophage NO production. Especially, aryl carbamates 10 and 11 exhibited more potent inhibitory activity against COX-2 and PGF 1 production.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2012.03.028

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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