Pascal Verdie

Publications (4)8.6 Total impact

• Article: The pipecolic linker—an acid-labile handle for derivatization of secondary amines on a solid-support. Part 3

  Paweł Zajdel, Nicolas Masurier, Vittorio Canale, Pascal Verdie, Muriel Amblard, Maciej Pawłowski, Jean Martinez, Gilles Subra
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  ABSTRACT: Herein, we demonstrate the versatility of the pipecolic linker for the structural diversification of secondary amines with potential CNS activity. The solid-phase methods elaborated involved N1-indole sulfonylation, nitroindole and nitroarene reduction, and microwave-assisted Buchwald–Hartwig N-arylation.
  Tetrahedron Letters 01/2013; 54(8):998-1002. · 2.68 Impact Factor
• Article: Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.

  Paweł Zajdel, Gilles Subra, Pascal Verdie, Ewa Gabzdyl, Andrzej J Bojarski, Beata Duszyńska, Jean Martinez, Maciej Pawłowski
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  ABSTRACT: A series of arylsulfonamides containing guanidine incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT(1A), 5-HT(2A), and 5-HT(7) receptors. The results demonstrated that N-alkyl-N'-dialkylguanidines displayed good 5-HT(7)/5-HT(1A) selectivity and may be regarded as promising structural core for development of 5-HT(7) ligands.
  Bioorganic & medicinal chemistry letters 07/2009; 19(16):4827-31. · 2.65 Impact Factor
• Article: The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones.

  Paweł Zajdel, Gilles Subra, Pascal Verdie, Andrzej J Bojarski, Beata Duszyńska, Katarzyna Basista, Jolanta Obniska, Jean Martinez, Maciej Pawłowski
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  ABSTRACT: A library of ethylene analogs of the previously described arylpiperazines with N-acylated amino acids was synthesized on SynPhase Lanterns and the library representatives were evaluated for their 5-HT(1A) and 5-HT(2A) receptor affinities. The obtained results were compared with those reported for compounds containing propylene and a butylene spacer and they revealed that 5-HT(1A) receptor affinity decreased proportionally with the length of the alkyl chain. Furthermore, the synthesized 3-cycloalkyl derivatives containing two methylene group spacers showed that the 3-position of pyrrolidine-2,5-dione preferred substituents of hydrophobic character.
  European journal of medicinal chemistry 08/2008; 44(2):800-8. · 3.27 Impact Factor
• Article: The influence of an ethylene spacer on the 5-HT1A and 5-HT2A receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones

  Paweł Zajdel, Gilles Subra, Pascal Verdie, Andrzej J. Bojarski, Beata Duszyńska, Katarzyna Basista, Jolanta Obniska, Jean Martinez, Maciej Pawłowski
  [show abstract] [hide abstract]
  ABSTRACT: A library of ethylene analogs of the previously described arylpiperazines with N-acylated amino acids was synthesized on SynPhase™ Lanterns and the library representatives were evaluated for their 5-HT1A and 5-HT2A receptor affinities. The obtained results were compared with those reported for compounds containing propylene and a butylene spacer and they revealed that 5-HT1A receptor affinity decreased proportionally with the length of the alkyl chain. Furthermore, the synthesized 3-cycloalkyl derivatives containing two methylene group spacers (20, 21) showed that the 3-position of pyrrolidine-2,5-dione preferred substituents of hydrophobic character.Graphical abstract
  European Journal of Medicinal Chemistry. 44(2):800-808.