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  • Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.

Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.

Journal of medicinal chemistry (2006-02-03)
Yasuhiro Goto, Sachie Arai-Otsuki, Yukari Tachibana, Daisuke Ichikawa, Satoshi Ozaki, Hiroyuki Takahashi, Yoshikazu Iwasawa, Osamu Okamoto, Shoki Okuda, Hisashi Ohta, Takeshi Sagara
RESUMEN

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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L-Prolinamide, 98%