Benzofuran based PDE4 inhibitors.

Autor: McGarry DG; Department of Medicinal Chemistry, Rhône Poulenc Rorer, Collegeville, PA 19426, USA., Regan JR, Volz FA, Hulme C, Moriarty KJ, Djuric SW, Souness JE, Miller BE, Travis JJ, Sweeney DM
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 1999 Jun; Vol. 7 (6), pp. 1131-9.
DOI: 10.1016/s0968-0896(99)00038-3
Abstrakt: Replacement of the 3,4-dialkoxyphenyl substructure common to a number of PDE4 inhibitors with a 2-alkyl-7-methoxybenzofuran unit is described. This substitution can result in either enhancement or substantial reductions in PDE4 inhibitory activity depending on the system to which it is applied. An in vitro SAR study of a potent series of 4-(2-heteroaryl-ethyl)-benzoiurans 26 is also presented.
Databáze: MEDLINE