Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group

Ferrocene analogues of the antiinflammatory agents tolmetin (1), fenbufen (2), flurbiprofen (3), and fenclofenac (4) were synthesized and tested for biological activity. The derivatives exhibited little or no antiarthritic or platelet antiaggregatory activity, indicating that the ferrocene moiety is...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 26; no. 2; pp. 226 - 229
Main Authors:	Maryanoff, Bruce E, Keeley, Stanley L, Persico, Frank J
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 01-02-1983
Subjects:	Animals Anti-Inflammatory Agents - chemical synthesis Arthritis, Experimental - drug therapy Blood Platelets - drug effects Blood Platelets - metabolism Female Ferrous Compounds - chemical synthesis Ferrous Compounds - pharmacology Ferrous Compounds - therapeutic use Humans Iron - chemical synthesis Metallocenes Organometallic Compounds - chemical synthesis Organometallic Compounds - pharmacology Organometallic Compounds - therapeutic use Platelet Aggregation - drug effects Rats Rats, Inbred Strains Serotonin - blood Serotonin - metabolism Structure-Activity Relationship
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Summary:	Ferrocene analogues of the antiinflammatory agents tolmetin (1), fenbufen (2), flurbiprofen (3), and fenclofenac (4) were synthesized and tested for biological activity. The derivatives exhibited little or no antiarthritic or platelet antiaggregatory activity, indicating that the ferrocene moiety is a poor bioisostere for aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents.
Bibliography:	ark:/67375/TPS-KRTXPWT6-K istex:5AE3A00EF9E21A02867790A299C8EB901D4DD4F5 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00356a020