1.
Bioorg Med Chem Lett
; 16(21): 5691-4, 2006 Nov 01.
Article
in English
| MEDLINE
| ID: mdl-16931005
ABSTRACT
The synthesis and biological evaluation of a series of benzimidazolone beta(3) adrenergic receptor agonists are described. A trend toward the reduction of rat atrial tachycardia upon increasing steric bulk at the 3-position of the benzimidazolone moiety was observed.
Subject(s)
Adrenergic beta-3 Receptor Antagonists , Adrenergic beta-Agonists/pharmacology , Benzimidazoles/pharmacology , Adrenergic beta-Agonists/chemistry , Benzimidazoles/chemistry , Humans
2.
Bioorg Med Chem Lett
; 16(13): 3415-8, 2006 Jul 01.
Article
in English
| MEDLINE
| ID: mdl-16677814
ABSTRACT
The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported.