Synthesis and structure–activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: Application of weakly basic sulfoximine …

…, A Rath, V Unadkat, B Sharma, H Ajani, J Kumar…

文献索引：Pandya, Vrajesh; Jain, Mukul; Chakrabarti, Ganes; Soni, Hitesh; Parmar, Bhavesh; Chaugule, Balaji; Patel, Jigar; Jarag, Tushar; Joshi, Jignesh; Joshi, Nirav; Rath, Akshyaya; Unadkat, Vishal; Sharma, Bhavesh; Ajani, Haresh; Kumar, Jeevan; Sairam, Kalapatapu V.V.M.; Patel, Harilal; Patel, Pankaj European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 136 - 152

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被引用次数: 15

摘要

A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead optimization at this novel P4 group led to many potent factor Xa inhibitors with excellent anticoagulant activity in human plasma. Selected compounds were dosed orally in rats and checked for their ex vivo prothrombin time prolonging activity, which resulted in ...