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

  • Lee, Bit
  • Kwak, Jae-Hwan
  • Huang, Shin-Won
  • Jang, Jae-Yong
  • Lim, Sanglae
  • ... Lee, Kiho
  • 외 8명
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초록

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. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

키워드

4-O-MethylhonokiolCyclooxygenase-2 (COX-2)Aryl carbamateIsoxazoleTriazoleONE-POT SYNTHESISMAGNOLIA-OFFICINALISMEMORY IMPAIRMENTETHANOL EXTRACT1,2,3-TRIAZOLESCONSTITUENTSOBOVATOLDISEASE
제목
Design and synthesis of 4-O-methylhonokiol analogs as inhibitors of cyclooxygenase-2 (COX-2) and PGF(1) production
저자
Lee, BitKwak, Jae-HwanHuang, Shin-WonJang, Jae-YongLim, SanglaeKwak, Young-ShinLee, KihoKim, Hyung SookHan, Sang-BaeHong, Jin-TaeLee, HeesoonSong, SukgilSeo, Seung-YongJung, Jae-Kyung
DOI
10.1016/j.bmc.2012.03.028
발행일
2012-05-01
유형
Article
저널명
Bioorganic & Medicinal Chemistry
20
9
페이지
2860 ~ 2868