Studies on Topical Antiinflammatory Agents. I. ; Synthesis and Vasoconstrictive Activity of Corticosteroid 17-Succinyl Esters

A series of 17-succinyl derivatives of four corticosteroids was prepared. They were tested for vasoconstrictive activity in humans, using 9α-fluoro-11β, 21-dihydroxy-16β-methyl-17α-valeryloxy-1, 4-pregnediene-3, 20-dione (betamethasone 17-valerate, BV) as a standard. The activities of the 21-chloro...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1989/06/25, Vol.37(6), pp.1534-1539
Hauptverfasser:	MITSUKUCHI, Morihiro, NAKAGAMI, Jozi, IKEMOTO, Tomoyuki, HIGUCHI, Shohei, TARUMOTO, Yasuo, YASUI, Hajime, SOTA, Kaoru
Format:	Artikel
Sprache:	eng
Schlagworte:	21-chloro-17α-(3-methoxycarbonyl)propanoyloxy corticosteroid Administration, Topical Alicyclic compounds, terpenoids, prostaglandins, steroids Animals Anti-Inflammatory Agents - chemical synthesis Anti-Inflammatory Agents - pharmacology antiinflammatory agent Betamethasone Valerate - pharmacology Chemical Phenomena Chemistry corticosteroid Exact sciences and technology Organic chemistry Preparations and properties Rabbits Steroids Structure-Activity Relationship vasoconstrictive activiry Vasoconstrictor Agents - chemical synthesis
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Zusammenfassung:	A series of 17-succinyl derivatives of four corticosteroids was prepared. They were tested for vasoconstrictive activity in humans, using 9α-fluoro-11β, 21-dihydroxy-16β-methyl-17α-valeryloxy-1, 4-pregnediene-3, 20-dione (betamethasone 17-valerate, BV) as a standard. The activities of the 21-chloro 17-methylsuccinate compounds (6A, 6C and 6D) were greater than that of BV. A structure-activity relationship study showed that the activities of the 21-chloro 17-methylsuccinates were more potent than those of the corresponding 21-esters.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.37.1534