A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.06.061 | DOI Listing |
Publication Analysis
Top Keywords
analogues mch
8
antagonist sb-568849
8
discovery potent
4
potent stable
4
stable conformationally
4
conformationally constrained
4
constrained analogues
4
mch antagonist
4
sb-568849 strategy
4
strategy systematically
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!