185406-76-2Relevant articles and documents
Dihydrobenzofurans
-
, (2008/06/13)
Compounds of formula I, wherein Het represents a heterocycle having the meaning and R1, R2, R3 and R4 have the meanings as given in the description are novel effective bronchial therapeutics.
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones
Van der Mey,Hatzelmann,Van Klink,Van der Laan,Sterk,Thibaut,Ulrich,Timmerman
, p. 2523 - 2535 (2007/10/03)
A series of 4-aryl-substituted cis-4a,5,8,8a-tetra- and cis-4a,5,6,7,8,8a-hexahydro-2H-phthalazin-1-ones with high inhibitory activity toward cAMP-specific phosphodiesterase (PDE4) was synthesized. To study structure-activity relationships various substituents were introduced to the 2-, 3-, and 4-positions of the 4-phenyl ring. Substitution at the 4-position of the phenyl ring was restricted to a methoxy group, probably due to unfavorable steric interactions of larger groups with the binding site. The introduction of many alkoxy substituents including distinct ring systems and functional groups was allowed to the 3-position. It was found that in general the cis-4a,5,8,8a-tetrahydro-2H-phthalazin-1-ones are more potent than their hexahydrophthalic counterparts, the best activity residing in (4-imidazol-1-yl-phenoxy)butoxy analogue 16o (pIC50 = 9.7).
