New generation dopaminergic agents. 3. Accessing the D2 pharmacophore via the 7-hydroxy-2-aminomethyl benzoxazine moiety

Medicinal Chemistry Research

Volumn 7, Issue 8, 1997, Pages 429-435

  Mewshaw, Richard E ^a   Shi, Xiaojie ^a   Mazandarani, Hossein ^a   Coupet, Joseph ^a   McGaughey, Georgia B ^a   Andree, Terrance H ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 0010458851     PISSN: 10542523     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (8)

1. For Part 2 see Mewshaw, R. E.; Shi, X.; Mazandarani, H.; Coupet, J.; McGaughey, G.; Andree, T. Bioorg. Chem. Med. Lett. 1998, (in press).
2. For Part 1 see Mewshaw, R. E.; Kavanagh, J.; Stack, G.; Marquis, K.; Shi, X.; Kagan, M. Z.; Webb, M. B.; Katz, A. H.; Park, A.; Kang, Y. H.; Abou-Gharbia, M.; Scerni, R.; Wasik, T.; Cortes-Burgos, L.; Spangler, T.; Brennan, J. A.; Pielsa, M.; Mazandarani, H.; Cockett, M. I.; Ochalski, R.; Coupet, J.; Andree, T. J. Med. Chem. 1997, 40, 4235.
3. Lahti, R. A.; Figur, L. M.; Peircey, M. F.; Ruppel, P. L.; Evans, D. L. Mol. Pharm. 1992, 42, 432.
4. Wasik, T.; Cockett, M.; Andree, T. H. Soc. Neurosci. Abst. 22: 831, 1996.
5. i values are the means of n = 2-3 experiments run at nine different concentrations. Each experiment was carried out in triplicate. 95% confidence limits were generally <± 15 % of the mean value.
6. McDermed, J. D. ; Freeman, H. S. Catecholamines: Basic and Clinical Frontiers; Usdin, E., Kopin, I., Barchas, J., Eds. ; Pergamon: New York, 1979; Vol. 1, p 568.
7. pKa calculations were performed using the CompuDrug software package version 3.1 (Chemistry Ltd., pKalc).
8. Cheng, Y. C.; Prusoff, W. H. Biochem. Pharmacol. 1973, 33, 3099.