ArticleACS medicinal chemistry letters2011
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
5 citing papers in PubMed.
- Vasoinhibin is Generated by the Renin-angiotensin System.Endocrinology · 2025Article
- Metal-free C(spChemical science · 2021Article
- Rapid functionalization of multiple C-H bonds in unprotected alicyclic amines.Nature chemistry · 2020Article
- Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations.Bioorganic & medicinal chemistry · 2017Article
- Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.ACS medicinal chemistry letters · 2012Article
Corrections and comments
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Authors and funding
20 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)methyl group and utilization of a different attachment point led to the identification of clinical candidate 9. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans.
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Registered trials
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