Alzheimer's disease is a grave social problem in an ageing population. A major problem is the passage of drugs through the blood-brain barrier. This work tests the hypothesis that the conjugation of peptidomimetic β-secretase inhibitors with a fragment of Amyloid-β peptide facilitates entrance into the Central Nervous System. HVR-3 (compound 4), one of the conjugation products, was found to be as potent as OM00-3, a known peptidomimetic inhibitor, four-fold more selective towards β-secretase 1 in relation to β-secretase 2 and three-fold more resistant to in vitro metabolization in Human serum. Its intravenous administration to mice and Wistar rats generated an active metabolite recovered from the rodent's brains.