Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595174 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Based on in house screening lead compound 1 for the NAR project, SAR studies have been focused on the modification of the C2 ethers of the pyrimidinedione core structure. In this effort, an unpredictable SAR trend was overcome in the alkyl ether and arylalkyl ether series to identify compound 24 with improved in vitro activity compared to nicotinic acid. More consistent and predictable SAR was achieved in the propargyl ether series. Lead compound 41 was identified with good in vitro and in vivo activity in rat, and much improved rat PK profile.
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Authors
Xianhai Huang, Jing Su, Ashwin U. Rao, Haiqun Tang, Wei Zhou, Xiaohong Zhu, Xiao Chen, Zhidan Liu, Ying Huang, Sylvia Degrado, Dong Xiao, Jun Qin, Robert Aslanian, Brian A. McKittrick, Scott Greenfeder, Margaret van Heek, Madhu Chintala, Anandan Palani,