Cyclooxygenase-1 and cyclooxygenase-2 inhibition of novel 1,2-disubstituted imidazoles.
Novel 1,2-disubstituted imidazoles were synthesized and tested for COX-1 and COX-2 inhibition. A substituted phenyl cycle in position 1 and an alicyclic tertiary alcohol in position 2 gave COX-1-selective compounds with potency and selectivity depending on the different substituents.
Handler
Norbert
N
Department of Medicinal Chemistry, University of Vienna, Vienna, Austria.
Jaeger
Walter
W
Kuen-Krismer
Bea
B
Erker
Thomas
T
D000818:Animals; D051545:Cyclooxygenase 1 / Q000378:metabolism*; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007093:Imidazoles; D007527:Isoenzymes; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2