New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: High affinity ligands for the α1-adrenoceptor subtypes

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 24, 2006, Pages 6200-6203

  Romeo, Giuseppe ^a   Materia, Luisa ^a   Marucci, Gabriella ^b   Modica, Maria ^a   Pittalà, Valeria ^a   Salerno, Loredana ^a   Siracusa, Maria Angela ^a   Buccioni, Michela ^b   Angeli, Piero ^b   Minneman, Kenneth P ^c  

^a UNIVERSITY OF CATANIA   (Italy)

^b UNIVERSITY OF CAMERINO   (Italy)

^c EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

1 Adrenoceptor; 1D Adrenoceptor subtype; Antagonist; Ligand; Synthesis

Indexed keywords

ALPHA 1 ADRENERGIC RECEPTOR; ALPHA 1 ADRENERGIC RECEPTOR BLOCKING AGENT; INDOLE DERIVATIVE; PYRIMIDINE DERIVATIVE; RECEPTOR SUBTYPE;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CHEMICAL STRUCTURE; CONTROLLED STUDY; DRUG POTENCY; DRUG SYNTHESIS; EMBRYO; HUMAN; HUMAN CELL; NONHUMAN; RAT;

ANIMALS; INDOLES; LIGANDS; MALE; PROSTATE; PYRIMIDINES; RATS; RECEPTORS, ADRENERGIC, ALPHA-1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33750682324     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.09.034     Document Type: Article

References (19)

1. Hieble J.P., Bylund D.B., Clarke D.E., Eikenburg D.C., Langer S.Z., Lefkowitz R.J., Minneman K.P., and Ruffolo Jr. R.R. Pharmacol. Rev. 47 (1995) 267
2. Romeo G., Materia L., Salerno L., Russo F., and Minneman K.P. Expert Opin. Ther. Patents 14 (2004) 619
3. Leonardi A., Hieble J.H., Guarneri L., Naselsky D.P., Poggesi E., Sironi A., Sulpizio A.C., and Testa R. J. Pharmacol. Exp. Ther. 281 (1997) 1272
4. Swinn D.A. BJU Int. 86 (2000) 11
5. Hancock A.A., Buchner S.A., Bruner M.E., Esbenshade T.A., Ireland L.M., Katwala S., Milicic I., Meyer M.D., Kerwin J.F., and Williams M. J. Pharmacol. Exp. Ther. 300 (2002) 478
6. Russo F., Romeo G., Guccione S., and De Blasi A. J. Med. Chem. 34 (1991) 1850
7. Romeo G., Ambrosini D., Guccione S., De Blasi A., and Russo F. Eur. J. Med. Chem. 24 (1993) 499
8. Romeo G., Russo F., Guccione S., Barbarulo D., and De Blasi A. Farmaco 50 (1995) 471
9. Romeo G., Russo F., and De Blasi A. J. Heterocycl. Chem. 38 (2001) 391
10. Romeo G., Materia L., Manetti F., Cagnotto A., Mennini T., Nicoletti F., Botta M., Russo F., and Minneman K.P. J. Med. Chem. 46 (2003) 2877
11. Leonardi A., Barlocco D., Montesano F., Cignarella G., Motta G., Testa R., Poggesi E., Seeber M., De Benedetti P.G., and Fanelli F. J. Med. Chem. 47 (2004) 1900
12. Konkel M.J., Wetzel J.M., Cahir M., Craig D.A., Noble S.A., and Gluchowski C. J. Med. Chem. 48 (2005) 3076
13. 1-(5-Chloro-2-methoxyphenyl)piperazine (6) was a gift of Clariant Life Science Molecules (France) S.A.S.
14. 2).
15. 2).
16. Rosini M., Antonello A., Cavalla A., Bolognesi M.L., Minarini A., Marucci G., Poggesi E., Leonardi A., and Melchiorre C. J. Med. Chem. 46 (2003) 4895
17. Van Rossum J.M. Arch. Int. Pharmacodyn. 143 (1963) 299
18. Uberti M.A., Hall R.A., and Minneman K.P. Mol. Pharmacol. 64 (2003) 1379
19. George S.R., O'Dowd B.F., and Lee S.P. Nat. Rev. Drug Discov. 1 (2002) 808