1.
Bioorg Med Chem Lett
; 17(14): 3910-5, 2007 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-17502143
ABSTRACT
We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure-activity relationships of 2 and 3 along with dog pharmacokinetic results are described.
Subject(s)
Amides/pharmacology , Amyloid Precursor Protein Secretases/antagonists & inhibitors , Azepines/chemistry , Azepines/pharmacology , Azepines/chemical synthesis , Cyclization , Models, Molecular , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 15(1): 29-35, 2005 Jan 03.
Article
in English
| MEDLINE
| ID: mdl-15582405
ABSTRACT
Syntheses and SAR studies of 5-amidinobenzo[b]thiophene analogs provided compounds with low submicromolar factor IXa activity and equal or slightly better selectivity relative to factor Xa.
Subject(s)
Factor IXa/antagonists & inhibitors , Factor Xa Inhibitors , Serine Proteinase Inhibitors/pharmacology , Thiophenes/pharmacology , Serine Proteinase Inhibitors/chemistry , Structure-Activity Relationship , Thiophenes/chemistry
3.
Bioorg Med Chem Lett
; 14(21): 5269-73, 2004 Nov 01.
Article
in English
| MEDLINE
| ID: mdl-15454209
ABSTRACT
Structural features of a 5-amidinoindole inhibitor of factor Xa, which displayed modest inhibition of factor IXa were varied to increase potency and improve selectivity for factor IXa.
