Literature DB >> 17088069

Design, synthesis, and SAR analysis of novel selective sigma1 ligands.

Simona Collina1, Guya Loddo, Mariangela Urbano, Laura Linati, Athos Callegari, Francesco Ortuso, Stefano Alcaro, Christian Laggner, Thierry Langer, Orazio Prezzavento, Giuseppe Ronsisvalle, Ornella Azzolina.   

Abstract

A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma(1) and sigma(2) receptors. Many compounds exhibited nanomolar affinity for sigma(1) subtype receptor with good selectivity over sigma(2). A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.

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Year:  2006        PMID: 17088069     DOI: 10.1016/j.bmc.2006.10.048

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors.

Authors:  Abdol R Hajipour; Dominique Fontanilla; Uyen B Chu; Marty Arbabian; Arnold E Ruoho
Journal:  Bioorg Med Chem       Date:  2010-04-29       Impact factor: 3.641

2.  Pharmacology and therapeutic potential of sigma(1) receptor ligands.

Authors:  E J Cobos; J M Entrena; F R Nieto; C M Cendán; E Del Pozo
Journal:  Curr Neuropharmacol       Date:  2008-12       Impact factor: 7.363

3.  Novel Enantiopure Sigma Receptor Modulators: Quick (Semi-)Preparative Chiral Resolution via HPLC and Absolute Configuration Assignment.

Authors:  Marta Rui; Annamaria Marra; Vittorio Pace; Markus Juza; Daniela Rossi; Simona Collina
Journal:  Molecules       Date:  2016-09-10       Impact factor: 4.411

  3 in total

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