1.
Bioorg Med Chem Lett
; 14(18): 4607-13, 2004 Sep 20.
Article
in English
| MEDLINE
| ID: mdl-15324874
ABSTRACT
The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4.
Subject(s)
3',5'-Cyclic-AMP Phosphodiesterases/antagonists & inhibitors , Isoenzymes/antagonists & inhibitors , Phosphodiesterase Inhibitors/chemical synthesis , Phosphodiesterase Inhibitors/pharmacology , Thiadiazoles/chemical synthesis , Thiadiazoles/pharmacology , 3',5'-Cyclic-AMP Phosphodiesterases/metabolism , Cell Line , Cyclic Nucleotide Phosphodiesterases, Type 4 , Cyclic Nucleotide Phosphodiesterases, Type 7 , Humans , Isoenzymes/metabolism , Phosphodiesterase Inhibitors/chemistry , Structure-Activity Relationship , Thiadiazoles/chemistry
2.
Org Lett
; 5(11): 2007-9, 2003 May 29.
Article
in English
| MEDLINE
| ID: mdl-12762708
ABSTRACT
[reaction: see text] A selective domino ring-closing metathesis (RCM)-cross-metathesis (CM) process between enynes and electron-deficient alkenes is reported. The conditions have been optimized for enynes 3 and methyl acrylate with catalyst IV. The scope and limitations of this reaction are described, and a possible mechanism is discussed.
