Identifying structural features on 1, 1-diphenyl-hexahydro-oxazolo [3, 4-a] pyrazin-3-ones critical for Neuropeptide S antagonist activity

…, BP Gilmour, HA Navarro, SP Runyon

文献索引：Zhang, Yanan; Gilmour, Brian P.; Navarro, Hernan A.; Runyon, Scott P. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 4064 - 4067

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被引用次数: 30

摘要

A series of 7-substituted 1, 1-diphenyl-hexahydro-oxazolo [3, 4-a] pyrazin-3-ones were synthesized and tested for Neuropeptide S (NPS) antagonist activity. A concise synthetic route was developed, which features a DMAP catalyzed carbamate formation. 4- Fluorobenzyl urea (1c) and benzyl urea (1d) were identified as the most potent antagonists among the compounds examined. Structure-activity relationships (SARs) demonstrate that ...