Generalized X-ray and neutron crystallographic analysis: more accurate and complete structures for biological macromolecules

Second-Generation Inhibitors for the Met

Second-Generation Inhibitors for the Metalloprotease Neprilysin Based on Bicyclic Heteroaromatic Scaffolds: Synthesis, Biological Activity, and X-Ray Crystal-Structure Analysis

✍ Stefan Sahli; Brian Frank; W. Bernd Schweizer; François Diederich; Denise Blum-K 📂 Article 📅 2005 🏛 John Wiley and Sons 🌐 German ⚖ 472 KB

## Abstract A new class of nonpeptidic inhibitors of the Zn^II^‐dependent metalloprotease neprilysin with __IC__~50~ values in the nanomolar activity range (0.034–0.30 μM) were developed based on structure‐based __de novo__ design (__Figs. 1__ and __2__). The inhibitors feature benzimidazole and im