Abstract
Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT(1) and MT(2) receptors are reported. Compounds 11f and 18b (MT(1)/MT(2) agonist) have human microsomal intrinsic clearance comparable to ramelteon.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
-
Amides / chemical synthesis
-
Amides / chemistry*
-
Amides / pharmacology
-
Animals
-
Cyclopropanes / chemical synthesis*
-
Cyclopropanes / chemistry
-
Cyclopropanes / pharmacology
-
Drug Design
-
Humans
-
Ligands
-
Microsomes / metabolism
-
Piperidines / chemical synthesis*
-
Piperidines / chemistry
-
Piperidines / pharmacology
-
Rats
-
Receptor, Melatonin, MT1 / agonists*
-
Receptor, Melatonin, MT1 / metabolism
-
Receptor, Melatonin, MT2 / agonists*
-
Receptor, Melatonin, MT2 / metabolism
-
Structure-Activity Relationship
Substances
-
Amides
-
Cyclopropanes
-
Ligands
-
Piperidines
-
Receptor, Melatonin, MT1
-
Receptor, Melatonin, MT2