Abstract：
:The synthesis of a series of substituted heterocyclic alkoxypropionic acids is described. They were evaluated for antiinflammatory effects in two animal models of chronic inflammation; adjuvant arthritis and type II collagen arthritis in the rat. The desired profile of biological activity was characterized by the reduction of inflammation with the coincident restoration toward normal levels of the biochemical markers (acute phase proteins) associated with the inflammatory response, an effect that was not shared by classical nonsteroidal antiinflammatory agents. Romazarit, (Ro 31-3948, 7), 2-[[2-(4-chlorophenyl)-4-methyl-5-oxazolyl]methoxy]-2-methylpropio nic acid, was selected for further evaluation. In contrast to NSAIDs, romazarit was inactive in animal models of acute inflammation, and furthermore it did not inhibit the cyclooxygenase enzyme in vitro or in vivo. Inhibition of interleukin-1-mediated events in vitro has been observed.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Self CR,Barber WE,Machin PJ,Osbond JM,Smithen CE,Tong BP,Wickens JC,Bloxham DP,Bradshaw D,Cashin CHdoi
10.1021/jm00106a044subject
Has Abstract,Author List Incompletepub_date
1991-02-01 00:00:00pages
772-7issue
2eissn
0022-2623issn
1520-4804journal_volume
34pub_type
杂志文章abstract：:Imaging serotonin transporters (SERT) is an emerging research tool potentially useful to cast light on the mechanisms of drug action as well as to monitor the treatment of depressed patients. We have prepared two new derivatives of 3, 2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine (4) and 2-(2-(dimethylaminometh...
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更新日期：2012-04-12 00:00:00
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更新日期：1981-03-01 00:00:00
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