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  • Title: Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
    Author: Goto Y, Arai-Otsuki S, Tachibana Y, Ichikawa D, Ozaki S, Takahashi H, Iwasawa Y, Okamoto O, Okuda S, Ohta H, Sagara T.
    Journal: J Med Chem; 2006 Feb 09; 49(3):847-9. PubMed ID: 16451050.
    Abstract:
    A focused library approach identifying novel leads to develop a potent ORL1 antagonist is described. Beginning from a compound identified by random screening, an exploratory library that exhibited a diverse display of pharmacophores was designed. After evaluating ORL1 antagonistic activity, a highly focused library was designed based on 3D-pharmacophore similarity to known actives. A novel D-proline amide class was identified in this library and was found to possess potent ORL1 antagonistic activity.
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