1,2,4-Benzothiadiazine derivatives as α1 and 5-HT 1A receptor ligands

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 4, 2005, Pages 1185-1188

  Tait, Annalisa ^a   Luppi, Amedeo ^a   Franchini, Silvia ^a   Preziosi, Elisa ^a   Parenti, Carlo ^a   Buccioni, Michela ^b   Marucci, Gabriella ^b   Leonardi, Amedeo ^c   Poggesi, Elena ^c   Brasili, Livio ^a  

^a UNIVERSITY OF MODENA AND REGGIO EMILIA   (Italy)

^b UNIVERSITY OF CAMERINO   (Italy)

^c Recordati SpA   (Italy)

Author keywords

5 HT1A agonist; Arylpiperazine; Benzothiadiazine; 1D antagonist

Indexed keywords

ALPHA 1 ADRENERGIC RECEPTOR BLOCKING AGENT; BENZOTHIADIAZINE DERIVATIVE; SEROTONIN 1 AGONIST;

ARTICLE; BINDING AFFINITY; DRUG BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; STRUCTURE ANALYSIS;

EID: 20144387288     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.12.004     Document Type: Article

References (17)

1. R.R. Ruffolo, W. Bondinell, and J.P. Hieble J. Med. Chem. 38 1995 3681
2. R. Testa, C. Taddei, E. Poggesi, C. Destefani, S. Cotecchia, J.P. Hieble, A.C. Sulpizio, D. Naselsky, D. Bergsma, S. Ellis, A. Swift, S. Ganguly, R.R. Ruffolo, and A. Leonardi Pharmacol. Commun. 6 1995 79
3. D. Hoyer, D.E. Clarke, J.R. Fozard, P.R. Hartig, G.R. Martin, E.J. Mylecharane, P.R. Saxena, and P.P.A. Humpherey Pharmacol. Rev. 46 1994 157
4. C.L. Parks, P.S. Robinson, E. Sibille, T. Shenk, and M. Toth Proc. Natl. Acad. Sci. U.S.A. 95 1998 10734
5. I. Semkova, P. Wolz, and J. Krieglstein Eur. J. Pharmacol. 359 1998 251
6. S. Trumpp-Kallmeyer, J. Hoflack, A. Bruinvels, and M. Hibert J. Med. Chem. 35 1992 3448
7. M.L. López-Rodríguez, M.J. Morcillo, E. Fernández, E. Porras, L. Orensanz, M.E. Beneytez, J. Manzanares, and J.A. Fuentes J. Med. Chem. 44 2001 186
8. 3S (C, H, N). The free amine was transformed into the corresponding di-hydrochloride salt, which was crystallized from methanol/petroleum ether 60-80°C; mp 105°C
9. M. Eltze, R. Boer, K.H. Sanders, and N. Kolassa Eur. J. Pharmacol. 202 1991 33
10. S.A. Buckner, K.W. Oheim, P.A. Morse, S.M. Knepper, and A.A. Hancock Eur. J. Pharmacol. 297 1996 241
11. F.N. Ko, J.H. Guh, S.M. Yu, Y.S. Hou, Y.C. Wu, and C.M. Teng Br. J. Pharmacol. 112 1994 1174
12. R. Testa, L. Guarneri, E. Poggesi, P. Angelico, C. Velasco, M. Ibba, A. Cilia, G. Motta, C. Riva, and A. Leonardi J. Pharmacol. Exp. Ther. 290 1999 1258
13. M.L. López-Rodríguez, M.J. Morcillo, T.K. Rovat, E. Fernández, B. Vicente, A.M. Sanz, M. Hernández, and L. Orensanz J. Med. Chem. 42 1999 36
14. M.L. López-Rodríguez, M.J. Morcillo, T.K. Rovat, E. Fernández, A.M. Sanz, and L. Orensanz Bioorg. Med. Chem. Lett. 8 1998 581
15. J.A. Stanton, and M.S. Beer Eur. J. Pharmacol. 320 1997 267
16. A. De Lean, P.J. Munson, and D. Rodbar Am. J. Physiol. 235 1978 E97 E102
17. J.M. Van Rossum Arch. Int. Pharmacodyn. 143 1963 299