1.
Bioorg Med Chem Lett
; 21(10): 3163-7, 2011 May 15.
Article
in English
| MEDLINE
| ID: mdl-21458261
ABSTRACT
The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. Compounds 47 and 48 were found to be high affinity, selective vasopressin V(1A) antagonists.
Subject(s)
Amides/chemical synthesis , Amides/pharmacology , Antidiuretic Hormone Receptor Antagonists , Drug Discovery , Amides/chemistry , Aza Compounds/chemical synthesis , Aza Compounds/chemistry , Aza Compounds/pharmacology , Cells, Cultured , Cyclization , Humans , Liver/metabolism , Molecular Structure , Protein Binding/drug effects
2.
Bioorg Med Chem Lett
; 21(3): 932-5, 2011 Feb 01.
Article
in English
| MEDLINE
| ID: mdl-21227690
ABSTRACT
Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pk(a) of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pk(a) 6-8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.