1.
Bioorg Med Chem Lett
; 18(16): 4569-72, 2008 Aug 15.
Article
in English
| MEDLINE
| ID: mdl-18662879
ABSTRACT
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
Subject(s)
Amides/chemistry , Benzoxazines/pharmacology , Piperidines/chemistry , TRPV Cation Channels/antagonists & inhibitors , Benzoxazines/chemistry , Capsaicin/chemistry , Carrier Proteins/antagonists & inhibitors , Chemistry, Pharmaceutical/methods , Drug Design , Humans , Inhibitory Concentration 50 , Models, Chemical , Molecular Conformation , Protein Binding , Quantitative Structure-Activity Relationship , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 18(8): 2730-4, 2008 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-18359227
ABSTRACT
High throughput screening of our compound library revealed a series of N-pyridyl-3-benzamides as low micromolar agonists of the human TRPV1 receptor. Synthesis of analogs in this series led to the discovery of a series of N-quinolin-3-yl-benzamides as low nanomolar antagonists of human TRPV1.
