Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.
Thompson
Christopher F
CF
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christopher_thompson@merck.com <christopher_thompson@merck.com>
Quraishi
Nazia
N
Ali
Amjad
A
Tata
James R
JR
Hammond
Milton L
ML
Balkovec
James M
JM
Einstein
Monica
M
Ge
Lan
L
Harris
Georgianna
G
Kelly
Theresa M
TM
Mazur
Paul
P
Pandit
Shilpa
S
Santoro
Joseph
J
Sitlani
Ayesha
A
Wang
Chuanlin
C
Williamson
Joanne
J
Miller
Douglas K
DK
Yamin
Ting-ting D
TT
Thompson
Chris M
CM
O'Neill
Edward A
EA
Zaller
Dennis
D
Forrest
Michael J
MJ
Carballo-Jane
Ester
E
Luell
Silvi
S
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D005938:Glucocorticoids / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D051381:Rats; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D006571:Heterocyclic Compounds; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha