Synthesis and biological evaluation of 1,3,4-triaryl-3-pyrrolin-2-ones, a new class of selective cyclooxygenase-2 inhibitors.
The synthesis and structure activity relationships (SAR) of a series of novel selective COX-2 inhibitors are reported. The results show that some of the 1,3,4-triaryl-3-pyrrolin-2-ones 1 are more potent as COX-2 inhibitors than celecoxib, and that lactam Id has the same selectivity.
Bosch
J
J
Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Spain. jbosch@farmacia.far.ub.es
Roca
T
T
Catena
J L
JL
Llorens
O
O
Pérez
J J
JJ
Lagunas
C
C
Fernández
A G
AG
Miquel
I
I
Fernández-Serrat
A
A
Farrerons
C
C
D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004341:Drug Evaluation; D007527:Isoenzymes / Q000187:drug effects; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D011758:Pyrroles; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases