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trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.

Lorthiois E, Cumin F, Ehrhardt C, Kosaka T, Sellner H, Ostermann N, Francotte E, Wagner T, Maibaum J
Bioorg Med Chem Lett 25 1782-1786 (2015)
Cited: 2 times
EuropePMC logo PMID: 25782742

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.

Articles - 4ryc mentioned but not cited (2)

  1. Extensive Reliability Evaluation of Docking-Based Target-Fishing Strategies. Lapillo M, Tuccinardi T, Martinelli A, Macchia M, Giordano A, Poli G. Int J Mol Sci 20 E1023 (2019)
  2. Tiliroside Protects against Lipopolysaccharide-Induced Acute Kidney Injury via Intrarenal Renin-Angiotensin System in Mice. Yi X, Xu C, Yang J, Zhong C, Yang H, Tang L, Song S, Yu J. Int J Mol Sci 24 15556 (2023)




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