RT Journal Article
T1 One-pot cascade  synthesis of pyrazole based isosteres of valdecoxib by A [3+2] cycloaddition sequence and evaluation of their cox inhibitory activity
A1 Roscales García, Silvia
A1 Bechmann, Nicole
A1 Pietzsch, Jens
A1 Kniess, Torsten
AB A series of 5-methyl-3,4-diaryl-substituted 1H-pyrazoles, N-isosteres of valdecoxib, was synthesized by a [3+2] cycloaddition/[1,5] sigmatropic rearrangement sequence starting from tosylhydrazine, aryl methyl ketones and terminal aryl alkynes bearing various substituents (H, Me, OMe, F, SO2Me, SO2NH2). New pyrazoles were prepared regioselectively in a one-pot process with moderate-good yields. All compounds were used in in vitro cyclooxygenase (COX) assays to determine inhibitory potency and selectivity to COX-1 and COX-2. In general, these new pyrazoles are characterized by selective COX-2 inhibition activity in a micromolar range.
YR 2019
FD 2019
LK https://hdl.handle.net/20.500.14352/126401
UL https://hdl.handle.net/20.500.14352/126401
LA eng
NO HETEROCYCLES, Vol. 98, No. 3, 2019, pp. 416 - 428. © 2019 The Japan Institute of Heterocyclic Chemistry Received, 26th January, 2019, Accepted, 22nd February, 2019, Published online, 22nd March, 2019 DOI: 10.3987/COM-19-14048
DS Docta Complutense
RD 19 mar 2026