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Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors |
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| Authors: | Kuang Rongze Shue Ho-Jane Blythin David J Shih Neng-Yang Gu Danlin Chen Xiao Schwerdt John Lin Ling Ting Pauline C Zhu Xiaohong Aslanian Robert Piwinski John J Xiao Li Prelusky Daniel Wu Ping Zhang Ji Zhang Xiang Celly Chander S Minnicozzi Michael Billah Motasim Wang Peng |
| Affiliation: | Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. rongze.kuang@spcorp.com |
| Abstract: | Substituted quinolyl oxazoles were discovered as a novel and highly potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationship studies revealed that the oxazole core, with 4-carboxamide and 5-aminomethyl groups, is a novel PDE4 inhibitory pharmacophore. Selectivity profiles and in vivo biological activity are also reported. |
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