Chemical and Pharmaceutical Bulletin p. 692 - 697 (1990)
Update date:2022-08-04
Topics:
Mitsukuchi
Ikemoto
Taguchi
Higuchi
Abe
Yasui
Hatayama
As part of our search for new topical antiinflammatory agents, a series of corticosteroid 17-(alkylthio)- and methoxyalkanoate derivatives was prepared and tested for vasoconstrictive activities. Several compounds were proved to have activity superior or comparable to that of 9α-fluoro-11β,21-dihydroxy-16β-methyl-17α-valeryloxy-1,4- pregnadiene-3,20-dione (betamethasone 17-valerate, BV). Among these compounds, 21-chloro-11β-hydroxy-17α-(methylthio)acetoxy-4- pregnene-3,20-dione (5Aa) was found to have the most potent activity, being more active than BV. The structure-activity relationships of the series revealed that introduction of a (methylthio)acetate function into the 17-position as well as the 21-position of corticosteroids was effective for enhancing the topical antiinflammatory activity.
View MoreContact:+86-29-88710656
Address:South Tai bai Road, High Tech Development Zone, Xi'an China
Contact:0027-717-456976
Address:2ND FLOOR, 325 VAUSE ROAD, OVERPORT, 4001, SOUTH AFRICA
Guangzhou Reachin Chemical Co., Ltd
Contact:+86-20-37087379 ext.604
Address:A122C-1, Tianyuan Plaza, 401 Tianyuan Rd., Tianhe, Guangzhou, China
Contact:Tel: +86-25-58353800
Address:23 Lijing Road, Nanjing Hi-Tech Zone, Nanjing, Jiangsu, China, 210061
Changsha Yonta Industry Co., Ltd.
Contact:+ 86-731-8535 2228
Address:Rm.1717, North Bldg., No.368, East 2nd Ring Road(2nd Section)
Doi:10.1016/0022-328X(84)85065-2
(1984)Doi:10.1248/cpb.30.2732
(1982)Doi:10.1039/c8nj01455h
(2018)Doi:10.1039/c5ob02537k
(2016)Doi:10.1080/14756366.2019.1699553
(2020)Doi:10.1021/jacs.7b08496
(2017)