alexa Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).


Medicinal Chemistry

Author(s): Huber T, Manzenrieder F, Kuttruff CA, DornerCiossek C, Kessler H

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Abstract Cyclization of recently reported linear phosphino dipeptide isostere inhibitors of BACE1 via side chain olefin metathesis yielded macrocyclic BACE1 inhibitors. The most potent compound II-P1 (IC(50) of 47nM) and the corresponding linear analog I were tested for serum stability. The approach led to three times prolonged half life serum stability of 44min for the macrocyclic inhibitor II-P1 compared to the linear compound I. This article was published in Bioorg Med Chem Lett and referenced in Medicinal Chemistry

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