Abstract:
:A series of hydantoin prostaglandin analogues, in which the hexamethylene moiety of the acid side chain was replaced by other spacing groups possessing either ether, sulphide and/or olefin functionality, were prepared and evaluated for platelet aggregation inhibiting activity. The 4-thia analogue 13*) proved to be the most potent inhibitor (ca. 22x PGE1) and the 3-thia- and 3-oxa-analogues, 6 and 10 respectively, are approximately equipotent with BW245C (ca. 14x PGE1). Z-olefinic analogues (e.g. 11) were usually more potent than their E-isomers (e.g. 12). Structure-activity relationships are discussed in detail.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Barraclough P,Caldwell AG,Glen RC,Harris CJ,Stepney R,Whittaker N,Whittle BJdoi
10.1002/ardp.19933260206subject
Has Abstractpub_date
1993-02-01 00:00:00pages
85-95issue
2eissn
0365-6233issn
1521-4184journal_volume
326pub_type
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journal_title:Archiv der Pharmazie
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