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The Azulene Framework as a Novel Arene Bioisostere: Design of Potent Dopamine D4 Receptor Ligands Inducing Penile Erection |
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| Authors: | Stefan Löber Dr. Nuska Tschammer Dr. Harald Hübner Dr. Maria Rosaria Melis Prof. Dr. Antonio Argiolas Prof. Dr. Peter Gmeiner Prof. Dr. |
| Affiliation: | 1. Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, Schuhstra?e 19, 91052 Erlangen (Germany), Fax: (+49)?9131‐8522585, Homepage: medchem.uni‐erlangen.de;2. Bernard B. Brodie Department of Neuroscience, University of Cagliari, S.S. 554, km 4500, 09042 Monserrato, Cagliari (Italy) |
| Abstract: | Blue makes it happen : The non‐uniform charge distribution of the blue colored azulene framework is highly suitable for the bioisosteric replacement of bicyclic heteroarene moieties. Showing an analogous binding mode as heterocyclic dopamine D4 receptor‐selective lead compounds, the induction of penile erection in rats over a greater range of doses indicates a putative advantage of the rationally developed azulene derivative 2 b over apomorphine.  |
| Keywords: | agonists azulenes bioisosteres dopamine D4 receptors GPCR penile erection |