Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation
2012
A diverse library of carboxylic acids was synthesized on solid-support. The screening on hNEP identified a low molecular weight hit. Structure–activity relationships around the hit highlighted the critical role of configuration for both chiral centers. The path, that involves a side reaction, to the potent and selective NEP optimised inhibitor is presented.
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