Identification of a Novel Spiropiperidine Opioid Receptor-like 1 Antagonist Class by a Focused Library Approach Featuring 3D-Pharmacophore Similarity
Journal of Medicinal Chemistry2006Vol. 49(3), pp. 847–849
Citations Over TimeTop 15% of 2006 papers
Yasuhiro Gotô, Sachie Arai-Otsuki, Yukari Tachibana, Daisuke Ichikawa, Satoshi Ozaki, Hiroyuki Takahashi, Yoshikazu Iwasawa, Osamu Okamoto, Shoki Okuda, Hisashi Ohta, Takeshi Sagara
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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