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学科主题: 药学
题名:
Toward the development of chemoprevention agents. Part II: Chemo-enzymatic synthesis and anti-inflammatory activities of a new class of 5-amino-2-substitutedphenyl-1,3-dioxacycloalkanes
作者: Gu, Keli; Bi, Lanrong; Zhao, Ming; Wang, Chao; Ju, Jingfang; Peng, Shiqi
关键词: chemoprevention ; chemo-enzymatic synthesis ; 2,5-disubstituted-dioxacycloalkanes ; anti-inflammatory activity ; structure-activity ; relationship study
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2007-09-15
DOI: 10.1016/j.bmc.2007.06.018
卷: 15, 期:18, 页:6273-6290
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: PROSTAGLANDIN G/H SYNTHASE ; PENICILLIN-G ACYLASE ; KETOROLAC TROMETHAMINE ; COLORECTAL-CANCER ; DRUG TRANSPORT ; CACO-2 CELLS ; PERMEABILITY ; PREVENTION ; CHROMATOGRAPHY ; INFLAMMATION
英文摘要:

A new series of optically pure 5-amino-2-substitutedphenyl-1,3-dioxacyclozilkanes were designed and synthesized via a chemo-enzymatic combined method to develop new chemoprevention agents. Twenty-four of newly synthesized compounds significantly inhibited xylene-induced rat ear edema and exhibited comparable or better anti-inflammatory activities than the reference drug aspirin. Treatment of these anti-inflammatory agents did not prolong the tail bleeding time in rat. In addition, 5-amino-2-substitutedphenyl- I 3-dioxacycloalkanes exhibited good membrane permeability based on in vitro Caco-2 cell monolayer permeability assay. Furthermore, some preliminary structure-activity relationships were further analyzed among these compounds. Taken together, 5-amino-2-substitutedphenyl-1,3-dioxacycloalkanes may represent a new class of anti-inflammatory drugs with safer pharmacological profile. (c) 2007 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000249194900029
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57759
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Univ S Alabama, Mitchell Canc Inst, Mobile, AL 36688 USA
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100054, Peoples R China
3.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Gu, Keli,Bi, Lanrong,Zhao, Ming,et al. Toward the development of chemoprevention agents. Part II: Chemo-enzymatic synthesis and anti-inflammatory activities of a new class of 5-amino-2-substitutedphenyl-1,3-dioxacycloalkanes[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(18):6273-6290.
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