159748-56-8Relevant academic research and scientific papers
Design, synthesis and biological evaluation of indole derivatives as Vif inhibitors
Pu, Chunlan,Luo, Rong-Hua,Zhang, Mengqi,Hou, Xueyan,Yan, Guoyi,Luo, Jiang,Zheng, Yong-Tang,Li, Rui
, p. 4150 - 4155 (2017)
The crystal structure of viral infectivity factor (Vif) was reported recently, which makes it possible to design new inhibitors against Vif by structure-based drug design. Through analysis of the protein surface of Vif, the C2 pocket located in the N-terminal was found, which is suit for developing small molecular inhibitors. Then, in our article, fragment-based virtual screening (FBVS) was conducted and a series of fragments was obtained, among which, Zif-1 bearing indole scaffold and pyridine ring can form H-bonds with Tyr148 and Ile155. Subsequently, 19 derivatives of Zif-1 were synthesized. Through the immune-fluorescence staining and Western blot assays, Zif-15 shows potent activity in inhibiting Vif-mediated A3G degradation. Further docking experiment shows that Zif-15 form H-bond interactions with residues His139, Tyr148 and Ile155. Therefore, Zif-15 is a promising lead compound against Vif that can be used to treat AIDS.
Angiotensin II antagonists
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, (2008/06/13)
This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Angiotensin II antagonist intermediates
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, (2008/06/13)
This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
