N-Isoquinolin-5-yl-N′-aralkyl-urea and -amide antagonists of human vanilloid receptor 1

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 12, 2004, Pages 3053-3056

  Jetter, Michele C ^a   Youngman, Mark A ^a   McNally, James J ^a   Zhang, Sui Po ^a   Dubin, Adrienne E ^a   Nasser, Nadia ^a   Dax, Scott L ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Pain; Vanilloid; VR1 antagonists

Indexed keywords

ISOQUINOLINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; VANILLOID RECEPTOR 1 BLOCKING AGENT;

AGONIST; ARTICLE; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

AMIDES; CELL LINE; HUMANS; ISOQUINOLINES; RECEPTORS, DRUG; TRPV CATION CHANNELS; UREA;

EID: 2442543188     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.04.038     Document Type: Article

References (18)

1. Dax, S.; Dubin, A.; Jetter, M.; Nasser, N.; Shah, C.; Swanson, D.; Carruthers, N. I. Vanilloid Receptor Antagonists: Structure Activity Relationships via Parallel and Targeted Synthesis. In 17th International Symposium on Medicinal Chemistry, Barcelona, Spain, September 1-5, 2002
2. 7-Hydroxy-naphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1: McDonnell M.E., Zhang S.-P., Nasser N., Dubin A.E., Dax S.L. Bioorg. Med. Chem. Lett. 14:2004;531
3. Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor: McDonnell M.E., Zhang S.-P., Dubin A.E., Dax S.L. Bioorg. Med. Chem. Lett. 12:2002;1189
4. Codd, E.; Dax, S. L.; Jetter, M.; McDonnell, M.; McNally, J. J.; Youngman, M. WO 2003097586A1
5. TRPV1 Agonists and Antagonists: Appendino G., Munoz E., Fiebich B.L. Expert Opin. Ther. Pat. 13:2003;1825. and references cited therein
6. Small Molecules Targeting the Vanilloid Receptor Complex as Drugs for Inflammatory Pain: Planells-Cases R., Garcia-Martinez C., Royo M., Perez-Paya E., Carreno C., Messeguer F.A.A., Ferrer-Montiel A. Drugs Future. 28:2003;787. and references cited therein
7. Pomonis J.D., Harrison J.E., Mark L., Bristol D.R., Valenzano K.J., Walker K. J. Pharm. Exp. Ther. 306:2003;387
8. Walpole C.S., Wrigglesworth R., Bevan S., Campbell E.A., Dray A., James I.F., Perkins M.N., Reid D.J., Winter J. J. Med. Chem. 36:1993;2362
9. Walpole C.S., Wrigglesworth R., Bevan S., Campbell E.A., Dray A., James I.F., Masdin K.J., Perkins M.N., Winter J. J. Med. Chem. 36:1993;2373
10. Walpole C.S., Wrigglesworth R., Bevan S., Campbell E.A., Dray A., James I.F., Masdin K.J., Perkins M.N., Winter J. J. Med. Chem. 36:1993;2381
11. d)
12. 50 values
13. 3O, 332.101; found, 332.101
14. 3O, 346.117; found, 346.117
15. 3O, 360.132; found, 360.120
16. 2O, 344.3; found, 345.122
17. Brown, R. E.; Doughty, V. A.; Hollingworth, G. J.; Jones, A. B.; Lindon, M. J.; Moyes, C. R.; Rogers, L. WO 2003080578A1, 2003
18. Codd, E.; Dax, S. L.; Jetter, M.; McDonnell, M.; McNally, J. J.; Youngman, M. WO 2004007459A2, 2004