2-ARYLAZETINES AS LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS

Authors

  • Leonardo Degennaro Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro
  • Marina Zenzola Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro
  • Annunziatina Laurino Department of Neuroscience, Area del Farmaco e Salute del Bambino (NEUROFARBA)
  • Maria Maddalena Cavalluzzi Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro
  • Carlo Franchini Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro
  • Solomon Habtemariam Pharmacognosy Research Laboratories, Medway School of Science, University of Greenwich
  • Rosanna Matucci Department of Neuroscience, Area del Farmaco e Salute del Bambino (NEUROFARBA)
  • Renzo Luisi Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro
  • Giovanni Lentini Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

DOI:

https://doi.org/10.1007/3732

Keywords:

azetidine, ligand efficiency metrics, lipophilicity, neurodegeneration, nicotinic acetylcholine receptors, pain, schizophrenia, smoking cessation.

Abstract

Alternative and complementary procedures were adopted for preparing 2-arylazetidine derivatives in moderate to good yields. Preliminary biological evaluation of 2-arylazetidines as ligands of nicotinic acetylcholine receptors allowed to identify chloro-substituted analogs as the most interesting congeners. The title compounds may be considered as suitable hit compounds for developing new nicotinic acetylcholine receptor ligands that may be safer than the currently available drugs targeting nicotinic acetylcholine receptors. Our described synthetic approaches enable facile access to a large number of diversely decorated azetidines for studying the structure–activity relationships and for refining the toxico-pharmacological profile of these agents.

Author Biographies

Leonardo Degennaro, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

Marina Zenzola, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

Annunziatina Laurino, Department of Neuroscience, Area del Farmaco e Salute del Bambino (NEUROFARBA)

Maria Maddalena Cavalluzzi, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

Carlo Franchini, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

Solomon Habtemariam, Pharmacognosy Research Laboratories, Medway School of Science, University of Greenwich

Rosanna Matucci, Department of Neuroscience, Area del Farmaco e Salute del Bambino (NEUROFARBA)

Renzo Luisi, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

Giovanni Lentini, Department of Pharmacy – Drug Sciences, University of Studies of Bari Aldo Moro

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Published

2017-04-07

Issue

Vol. 53 No. 3 (2017): Privileged heterocyclic scaffolds in chemical biology and drug discovery: synthesis and bioactivity

Section

Original Papers