Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371041 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
Abstract
Recently, we reported on the discovery of (3S,4S)-disubstituted pyrrolidines (e.g., 2) as inhibitors of the human aspartyl protease renin. In our effort to further expand the scope of this novel class of direct renin inhibitors, a new sub-series was designed in which the prime site substituents are linked to the pyrrolidine core by a (3S)-amino functional group. In particular, analogs bearing the corresponding sulfonamide spacer (50, 51 and 54a) demonstrated a pronounced increase in in vitro potency compared to compound 2.
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Related Topics
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Organic Chemistry
Authors
Edwige Lorthiois, Frederic Cumin, Claus Ehrhardt, Takatoshi Kosaka, Holger Sellner, Nils Ostermann, Eric Francotte, Trixie Wagner, Jürgen Maibaum,