249583-83-3Relevant articles and documents
1-Imidazolylcarbonyloxy-substituted tetrahydroquinolines and pyridines: Synthesis and evaluation of P450 TxA2 inhibition
Hartmann, Rolf W.,Frotscher, Martin
, p. 358 - 362 (2007/10/03)
The title compounds are derived from our model describing structural requirements for strong P450 TxA2 inhibition. In the present paper the syntheses of the 1-imidazolylcarbonyloxy-substituted tetrahydroquinolines 1, 3, and 4, tetrahydro-naphthalene 2 and 3-ethylpyridines 5 and 6 are described. Using our P450 TxA2 inhibition assay, 1-6 were tested for enzyme inhibitory activity. Compound 1 (5-(1-imidazolylcarbonyloxy)-5,6,7,8- tetrahydroquinoline) turned out to be the most active derivative showing a potency similar to the reference compound dazoxiben (IC50 values 1.6 and 1.1 μM).