2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists |
| |
| Authors: | Shireman Brock T Dvorak Curt A Rudolph Dale A Bonaventure Pascal Nepomuceno Diane Dvorak Lisa Miller Kirsten L Lovenberg Timothy W Carruthers Nicholas I |
| |
| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. BShirema@prdus.jnj.com |
| |
| Abstract: | The synthesis and SAR for a novel series of 2-alkyl-4-aryl-tetrahydro-pyrido-pyrimidines and 2-alkyl-4-aryl-tetrahydro-pyrimido-azepines is described. Representative compounds were shown to be subtype selective 5-HT(2A) antagonists. Optimal placement of a basic nitrogen relative to the pyrimidine and the presence of a 4-fluorophenyl group in the pyrimidine 4-position was found to have a profound effect on affinity and selectivity. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
