Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.
A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11beta-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11beta-HSD2.
Kim
Se Hoan
SH
Department of Chemistry, Korea University, Seoul 121-742, Republic of Korea.
Ramu
Ravirala
R
Kwon
Sung Wook
SW
Lee
Su-Hee
SH
Kim
Chi Hyun
CH
Kang
Seung Kyu
SK
Rhee
Sang Dal
SD
Bae
Myung Ae
MA
Ahn
Sung Hoon
SH
Ha
Duck Chan
DC
Cheon
Hyae Gyeong
HG
Kim
Ki Young
KY
Ahn
Jin Hee
JH
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D051379:Mice; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
D013449:Sulfonamides; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1