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Volumn 8, Issue 24, 1998, Pages 3571-3576

Butyrophenone analogues in the carbazole series: Synthesis and determination of affinities at D2 and 5-HT(2A) receptors

Author keywords

[No Author keywords available]

Indexed keywords

BUTYROPHENONE DERIVATIVE; CLOZAPINE; DOPAMINE 2 RECEPTOR; HALOPERIDOL; NEUROLEPTIC AGENT; QF 2001B; QF 2002B; QF 2003B; QF 2004B; QF 2006B; QF 2014B; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

EID: 0032535552     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00639-8     Document Type: Article
Times cited : (12)

References (39)
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    • Antipsychotic agents
    • Wolf, M. E., Ed. 5th. edition. Therapeutic Agents. Wiley Interscience
    • 1. Martin, A. R. Antipsychotic Agents. In Burger's Medicinal Chemistry and Drug Discovery; Wolf, M. E., Ed. 5th. edition. Therapeutic Agents. Wiley Interscience, 1997; vol 5, p. 195.
    • (1997) Burger's Medicinal Chemistry and Drug Discovery , vol.5 , pp. 195
    • Martin, A.R.1
  • 2
    • 0344937935 scopus 로고
    • 2. (a) Seemann, P. Synapse 1987, 192, 481-483;
    • (1987) Synapse , vol.192 , pp. 481-483
    • Seemann, P.1
  • 4
    • 0025599851 scopus 로고
    • 3. For a review of pharmacological properties and therapeutic uses of clozapine see Fitton, A.; Heel, R. C. Drugs 1990, 40, 722
    • (1990) Drugs , vol.40 , pp. 722
    • Fitton, A.1    Heel, R.C.2
  • 23
    • 0344937931 scopus 로고    scopus 로고
    • note
    • 19. Compound QF 0510B does not produce catalepsy at dose as high as 20 mg/Kg.
  • 30
    • 0000414271 scopus 로고
    • 23. For the Fischer indolization mechanism, see: Hughes, D. L.; Zhao, D. J. Org. Chem. 1993, 58, 228.
    • (1993) J. Org. Chem. , vol.58 , pp. 228
    • Hughes, D.L.1    Zhao, D.2
  • 31
    • 0017916143 scopus 로고
    • 24. The 4-(p-fluorobenzoyl)piperidine fragment may be considered as a butyrophenone moiety constrained in a six-membered ring. The importance of this fragment on CNS agents acting compounds is well known. See, among others, (a) Boswell, R. F., Jr.; Welstead, W. J., Jr.; Duncan, R. L., Jr.; Johnson, D. N.; Funderburk, W. H. J. Med. Chem. 1978, 21, 136-138;
    • (1978) J. Med. Chem. , vol.21 , pp. 136-138
    • Boswell, R.F.J.1    Welstead W.J., Jr.2    Duncan R.L., Jr.3    Johnson, D.N.4    Funderburk, W.H.5
  • 34
    • 0028943137 scopus 로고
    • 2A receptor interactions. A key structural feature that may play a prominent role in these interactions would be the benzylic carbonyl group. Ismaiel, A. M.; Arruda, K.; Teitler, M.; Glennon, R. A. J. Med. Chem. 1995, 38, 1196-1202.
    • (1995) J. Med. Chem. , vol.38 , pp. 1196-1202
    • Ismaiel, A.M.1    Arruda, K.2    Teitler, M.3    Glennon, R.A.4
  • 37
    • 0344075890 scopus 로고    scopus 로고
    • note
    • 2O: C, 76.02%; H, 8.51%; N, 9.85%. Found: C, 76.30%; H, 8.63%; N, 9.57%.
  • 38
    • 0344075889 scopus 로고    scopus 로고
    • note
    • 13C-NMR, FTIR, MS). Yields given correspond to isolated pure compounds.


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