Literature DB >> 16085415

Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis.

Michael Brands1, Jens-Kerim Ergüden, Kentaro Hashimoto, Dirk Heimbach, Christian Schröder, Stephan Siegel, Johannes-Peter Stasch, Stefan Weigand.   

Abstract

A novel class of indole-based endothelin-converting enzyme (ECE) inhibitors was identified by high throughput screening. We report systematic optimization of this compound class by means of classical and solid-phase chemistry. Optimized compounds with a bisarylamide side chain at the 2-position of the indole skeleton exhibit low-nanomolar activity on ECE.

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Year:  2005        PMID: 16085415     DOI: 10.1016/j.bmcl.2005.06.085

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Pd/C-mediated synthesis of indoles in water.

Authors:  Mohosin Layek; Udaya Lakshmi; Dipak Kalita; Deepak Kumar Barange; Aminul Islam; K Mukkanti; Manojit Pal
Journal:  Beilstein J Org Chem       Date:  2009-09-23       Impact factor: 2.883

  1 in total

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