Bioorganic and Medicinal Chemistry Letters p. 983 - 987 (2004)
Update date:2022-08-05
Topics:
Zhang, Penglie
Bao, Liang
Zuckett, Jingmei F.
Goldman, Erick A.
Jia, Zhaozhong J.
Arfsten, Ann
Edwards, Susan
Sinha, Uma
Hutchaleelaha, Athiwat
Park, Gary
Lambing, Joseph L.
Hollenbach, Stanley J.
Scarborough, Robert M.
Zhu, Bing-Yan
Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity were performed at the central phenyl ring and at the S4 binding biphenyl region by incorporating water solublizing substituents. The resulting compounds (e.g., 7, 8, 14, 30a, and 32b) are highly potent in vitro, and show improved activity in human plasma-based thrombin generation assay.
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