Literature DB >> 15324876

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.

Edwige Lorthiois1, Patrick Bernardelli, Fabrice Vergne, Chrystelle Oliveira, Abdel-Kader Mafroud, Emmanuelle Proust, Lamia Heuze, François Moreau, Moulay Idrissi, Anita Tertre, Bernadette Bertin, Magali Coupe, Roger Wrigglesworth, Arnaud Descours, Patricia Soulard, Patrick Berna.   

Abstract

The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes.

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Year:  2004        PMID: 15324876     DOI: 10.1016/j.bmcl.2004.07.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Combined use of pharmacophoric models together with drug metabolism and genotoxicity "in silico" studies in the hit finding process.

Authors:  Ma José Jerez; Miguel Jerez; Coral González-García; Sara Ballester; Ana Castro
Journal:  J Comput Aided Mol Des       Date:  2013-01-08       Impact factor: 3.686

2.  Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice.

Authors:  Miriam Redondo; Valle Palomo; José Brea; Daniel I Pérez; Rocío Martín-Álvarez; Concepción Pérez; Nuria Paúl-Fernández; Santiago Conde; María Isabel Cadavid; María Isabel Loza; Guadalupe Mengod; Ana Martínez; Carmen Gil; Nuria E Campillo
Journal:  ACS Chem Neurosci       Date:  2012-08-08       Impact factor: 4.418

  2 in total

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