Triazole derivatives: A series of Darapladib analogues as orally active Lp-PLA 2 inhibitors

K Wang, W Xu, W Zhang, M Mo, Y Wang…

Index: Wang, Kai; Xu, Wenwei; Zhang, Wei; Mo, Mingguang; Wang, Yiping; Shen, Jianhua Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 10 p. 2897 - 2901

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Citation Number: 7

Abstract

This Letter reports our efforts towards the optimization of our previously identified series of imidazole and triazole derivatives that lead to the discovery of a series of orally active Lp- PLA2 inhibitors in C57 mice. These inhibitors are characterized by the presence of a diamine side chain in the molecules, such as 2c, 2f, and 4a. The introduction of the terminal- end amine succeeded in maintaining the in vitro activities at sub-nanomolar levels. The ...