New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 3, 1998, Pages 295-300

  Mewshaw, Richard E ^a   Husbands, Morris ^a   Gildersleeve, Elizabeth S ^a   Webb, Michael B ^a   Shi, Xiaojie ^a   Mazandarani, Hossein ^a   Cockett, Mark I ^a   Ochalski, Rafal ^a   Brennan, Julie A ^a   Abou Gharbia, Magid ^a   Marquis, Karen ^a   McGaughey, Georgia B ^a   Coupet, Joseph ^a   Andree, Terrance H ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DOPAMINE 2 RECEPTOR STIMULATING AGENT; DOPAMINE RECEPTOR; DOPAMINE RECEPTOR STIMULATING AGENT; PHENOXYETHYLAMINE DERIVATIVE; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CHEMICAL STRUCTURE; DRUG DESIGN; DRUG SYNTHESIS; NONHUMAN; RAT; REACTION ANALYSIS; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

DOPAMINE AGONISTS; PHENOLS; PIPERAZINES; RECEPTORS, DOPAMINE D2; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 0032477687     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00014-6     Document Type: Article

References (11)

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4. 4. 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.
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9. i values are the means of n = 2-3 experiments run at six different concentrations. Each experiment was carried out in triplicate. 95% confidence limits were generally ≤± 15 % of the mean value.
10. 10. All computations were performed using Sybyl software package version 6.3. The basic phenylpiperazine framework of 17 was identified from the Cambridge database and used as a starting point; further computations were performed using Sybyl v6.3.
11. 11. 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.