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 9 alpha-fluoro-11 beta, 21-dihydroxy-16 beta-methyl-17 alpha-valeryloxy-1,4-pregnadiene-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.
Mitsukuchi
M
M
Nakagami
J
J
Ikemoto
T
T
Higuchi
S
S
Tarumoto
Y
Y
Yasui
H
H
Sota
K
K
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001624:Betamethasone Valerate / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D011817:Rabbits; D013329:Structure-Activity Relationship; D014662:Vasoconstrictor Agents / Q000138:chemical synthesis*
D000893:Anti-Inflammatory Agents; D014662:Vasoconstrictor Agents; D001624:Betamethasone Valerate