These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors.
    Author: Scheiper B, Matter H, Steinhagen H, Stilz U, Böcskei Z, Fleury V, McCort G.
    Journal: Bioorg Med Chem Lett; 2010 Nov 01; 20(21):6268-72. PubMed ID: 20850300.
    Abstract:
    Selective inhibition of the aspartyl protease renin has gained attraction as an interesting approach to control hypertension and associated cardiovascular risk factors given its unique position in the renin-angiotensin system. Using a combination of high-throughput screening, parallel synthesis, X-ray crystallography and structure-based design, we identified and optimized a novel series of potent and non-chiral indole-3-carboxamides with remarkable potency for renin. The most potent compound 5k displays an IC(50) value of 2nM.
    [Abstract] [Full Text] [Related] [New Search]