Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.
The structure-activity relationships of some tetracyclic heterocycles related to Brequinar were explored. Activities as inhibitors of dihydroorotate dehydrogenase and the mixed lymphocyte reaction are related to ring system, heteroatom placement, and pendant ring substitution.
Pitts
W J
WJ
DuPont Merck Pharmaceutical Company, Wilmington, Delaware 19880-0500, USA.
Jetter
J W
JW
Pinto
D J
DJ
Orwat
M J
MJ
Batt
D G
DG
Sherk
S R
SR
Petraitis
J J
JJ
Jacobson
I C
IC
Copeland
R A
RA
Dowling
R L
RL
Jaffee
B D
BD
Gardner
T L
TL
Jones
E A
EA
Magolda
R L
RL
D001713:Biphenyl Compounds / Q000737:chemistry*; D000090722:Dihydroorotate Dehydrogenase; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry* / Q000494:pharmacology*; D007959:Lymphocyte Culture Test, Mixed; D010088:Oxidoreductases / Q000037:antagonists & inhibitors; D044925:Oxidoreductases Acting on CH-CH Group Donors; D013329:Structure-Activity Relationship; D011798:Quinaldines
D001713:Biphenyl Compounds; D000090722:Dihydroorotate Dehydrogenase; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D007166:Immunosuppressive Agents; D010088:Oxidoreductases; D044925:Oxidoreductases Acting on CH-CH Group Donors; C046943:brequinar; D011798:Quinaldines