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  1. AU="Roufos, I"
  2. AU="Ammad Ahmad Farooqi"
  3. AU="Zawadka-Kunikowska, Monika"
  4. AU="Young, A P"
  5. AU="Danielle M. Matriano"
  6. AU="Ancona, Jennifer"
  7. AU="Abdallah G. Kfoury"
  8. AU="Zaeske, C"
  9. AU="Hammerich, Kristoff"
  10. AU="Paul J. Burgess"
  11. AU="Valek, Lucie"
  12. AU="Mandal, Surajit"
  13. AU="Krumm, Laura"
  14. AU="Shimura, Hidetoshi"
  15. AU="Munguia-Lopez, Jose Gil"
  16. AU="Eysert, Fanny"
  17. AU="Qazi Arisa, Fakhar Ali"
  18. AU="Guan, Yunshan"
  19. AU="Ayachi, Jihene"
  20. AU="Boulvard Chollet, Xavier L E"
  21. AU="Kwon, Sohee"
  22. AU=Fra-Bido Sigrid
  23. AU="Delgado, Teresa Cardoso"
  24. AU="Judy Ly"
  25. AU="E Richtig"
  26. AU="Jones, D. C."
  27. AU="Revillet, Hélène" AU="Revillet, Hélène"
  28. AU="Lee, Ji Ye"
  29. AU="Yoshinaga, Kazuaki"
  30. AU="Moturi, Krishna"
  31. AU="Loizeau, J"
  32. AU="Gentry, Matthew S"
  33. AU="Drury, Lucy S"
  34. AU="Caraman, Irina"

Suchergebnis

Treffer 1 - 3 von insgesamt 3

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  1. Artikel: A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers.

    Roufos, I / Hays, S / Schwarz, R D

    Journal of medicinal chemistry

    1996  Band 39, Heft 7, Seite(n) 1514–1520

    Abstract: A structure-activity relationship study of a series of novel Na(+) channel blockers, structurally related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1, PD85639) is described. The diphenylacetic acid portion of the molecule ... ...

    Abstract A structure-activity relationship study of a series of novel Na(+) channel blockers, structurally related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1, PD85639) is described. The diphenylacetic acid portion of the molecule was left unchanged throughout the study, while structural features in the amine portion and the amide alkyl linkage of the molecule were modified. The compounds were tested for inhibition of veratridine-stimulated Na(+) influx in CHO cells expressing type IIA Na(+) channels. Several derivatives show a trend toward more potent Na+ channel blockade activity with increasing lipophilicity of the amine portion of the molecule. The presence of a phenyl ring near the amine increases inhibitory potency. A three-carbon spacer between the amide and amine is optimal, and a secondary amide linkage is preferred.
    Mesh-Begriff(e) Acetamides/chemical synthesis ; Acetamides/chemistry ; Acetamides/pharmacology ; Animals ; Benzeneacetamides ; CHO Cells ; Cricetinae ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Piperidines/chemistry ; Piperidines/pharmacology ; Sodium/metabolism ; Sodium Channel Blockers ; Sodium Channels/metabolism ; Structure-Activity Relationship ; Veratridine/pharmacology
    Chemische Substanzen Acetamides ; Benzeneacetamides ; Piperidines ; Sodium Channel Blockers ; Sodium Channels ; PD 85639 (150034-24-5) ; Veratridine (71-62-5) ; Sodium (9NEZ333N27)
    Sprache Englisch
    Erscheinungsdatum 1996-03-29
    Erscheinungsland United States
    Dokumenttyp Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm950467y
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel: Derivatives of 4-(2-N,N-di-n-propylaminoethyl)-5-hydroxyindole: synthesis and pharmacological effects.

    Cannon, J G / Roufos, I / Ma, S X / Long, J P

    Pharmaceutical research

    1992  Band 9, Heft 6, Seite(n) 735–738

    Abstract: 5-Methoxy-1-methyl-4-(2-N,N-di-n-propylaminoethyl)indole (12) was synthesized from 5-hydroxyindole by a multistep synthesis. This target compound was designed as a bioisostere of "p-dimethoxy" catechol congeners of dopaminergic agonists derived from a ... ...

    Abstract 5-Methoxy-1-methyl-4-(2-N,N-di-n-propylaminoethyl)indole (12) was synthesized from 5-hydroxyindole by a multistep synthesis. This target compound was designed as a bioisostere of "p-dimethoxy" catechol congeners of dopaminergic agonists derived from a variety of ring systems, in some of which p-dimethoxy-substituted systems are potent, active dopaminergic agonists. To complete the indole series, all possible combinations of N- and O-demethylated derivatives of 12 were prepared and were also evaluated pharmacologically. All members of this indole-derived series showed a low order of cardiovascular activity, which appeared to be independent of dopamine receptors. The lack of dopaminergic activity of 12 is cited as yet another example of the unpredictable effect of replacement of the catechol moiety of a dopaminergic agonist with a p-dimethoxy moiety.
    Mesh-Begriff(e) Animals ; Blood Pressure/drug effects ; Heart Rate/drug effects ; Indoles/chemical synthesis ; Indoles/pharmacology ; Male ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship
    Chemische Substanzen Indoles ; 4-(2-di-N-propylaminoethyl)indole (76149-15-0)
    Sprache Englisch
    Erscheinungsdatum 1992-06
    Erscheinungsland United States
    Dokumenttyp Journal Article
    ZDB-ID 843063-9
    ISSN 1573-904X ; 0724-8741 ; 0739-0742
    ISSN (online) 1573-904X
    ISSN 0724-8741 ; 0739-0742
    DOI 10.1023/a:1015839118825
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  3. Artikel: Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.

    Roufos, I / Hays, S J / Dooley, D J / Schwarz, R D / Campbell, G W / Probert, A W

    Journal of medicinal chemistry

    1994  Band 37, Heft 2, Seite(n) 268–274

    Abstract: The synthesis and structure-activity relationships of a series of phenylacetamides related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1) (PD85639) acting at the voltage-dependent Na+ channel are described. All structural ... ...

    Abstract The synthesis and structure-activity relationships of a series of phenylacetamides related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1) (PD85639) acting at the voltage-dependent Na+ channel are described. All structural variations for this study were made in the phenylacetic acid portion of these molecules, and the compounds were synthesized by coupling the appropriately substituted phenylacetic acid derivative with 3-[1-(2,6-dimethyl)piperidinyl]-propanamine using standard methods of amide formation. Compounds were tested as inhibitors of [3H]batrachtoxinin binding in rat neocortical membranes and also as inhibitors of veratridine-induced Na+ influx in Chinese hamster ovary cells expressing type IIA Na+ channels. Diphenylacetic acid derivatives with halogenated aromatic rings (12-15) were very potent in both assays, while alkoxy and alkyl substitution did not affect activity (16 and 17). Selected compounds were tested as potential neuroprotective agents in two cell culture assays involving inhibition of veratridine-induced and hypoxia-induced lactate dehydrogenase release. Compound 15 was equipotent with flunarizine, a reference compound in both neuroprotection assays.
    Mesh-Begriff(e) Acetamides/chemical synthesis ; Acetamides/pharmacology ; Animals ; Batrachotoxins/metabolism ; Benzeneacetamides ; CHO Cells ; Cell Hypoxia ; Cells, Cultured ; Cerebral Cortex/drug effects ; Cerebral Cortex/metabolism ; Cricetinae ; L-Lactate Dehydrogenase/metabolism ; Male ; Piperidines/chemistry ; Piperidines/pharmacology ; Rats ; Rats, Sprague-Dawley ; Sodium/metabolism ; Sodium Channel Blockers ; Structure-Activity Relationship ; Veratridine/antagonists & inhibitors ; Veratridine/pharmacology
    Chemische Substanzen Acetamides ; Batrachotoxins ; Benzeneacetamides ; Piperidines ; Sodium Channel Blockers ; PD 85639 (150034-24-5) ; Veratridine (71-62-5) ; Sodium (9NEZ333N27) ; L-Lactate Dehydrogenase (EC 1.1.1.27)
    Sprache Englisch
    Erscheinungsdatum 1994-01-21
    Erscheinungsland United States
    Dokumenttyp Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm00028a010
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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