Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application

DOI: 10.1016/j.bmcl.2009.11.092

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 603 - 607 (2010)

Update date:2022-07-30

Topics:

Authors:

Lerchner, Andreas

Machauer, Rainer

Betschart, Claudia

Veenstra, Siem

Rueeger, Heinrich

McCarthy, Clive

Tintelnot-Blomley, Marina

Jaton, Anne-Lise

Rabe, Sabine

Desrayaud, Sandrine

Enz, Albert

Staufenbiel, Matthias

Paganetti, Paolo

Rondeau, Jean-Michel

Neumann, Ulf

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Article abstract of DOI:10.1016/j.bmcl.2009.11.092

A series of macrocyclic peptidic BACE-1 inhibitors was designed. While potency on BACE-1 was rather high, the first set of compounds showed poor brain permeation and high efflux in the MDRI-MDCK assay. The replacement of the secondary benzylamino group wi

Full text of DOI:10.1016/j.bmcl.2009.11.092

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