Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2012 Jul 15;22(14):4740-4.
doi: 10.1016/j.bmcl.2012.05.072. Epub 2012 Jun 6.

Synthesis and Structure-Activity Relationship Studies of 1,3-disubstituted 2-propanols as BACE-1 Inhibitors

Affiliations

Synthesis and Structure-Activity Relationship Studies of 1,3-disubstituted 2-propanols as BACE-1 Inhibitors

Arun Babu Kumar et al. Bioorg Med Chem Lett. .

Abstract

A library of 1,3-disubstituted 2-propanols was synthesized and evaluated as low molecular weight probes for β-secretase inhibition. By screening a library of 121 1,3-disubstituted 2-propanol derivatives, we identified few compounds inhibiting the enzyme at low micromolar concentrations. The initial hits were optimized to yield a potent BACE-1 inhibitor exhibiting an IC(50) constant in the nanomolar range. Exploration of the pharmacological properties revealed that these small molecular inhibitors possessed a high selectivity over cathepsin D and desirable physicochemical properties beneficial to cross the blood-brain barrier.

Similar articles

See all similar articles

Cited by 1 article

Publication types

MeSH terms

LinkOut - more resources

Feedback