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Design and Synthesis of 2,3,5‐Substituted Imidazolidin‐4‐one Inhibitors of BACE‐1
Author(s) -
Barrow James C.,
Rittle Kenneth E.,
Ngo Phung L.,
Selnick Harold G.,
Graham Samuel L.,
Pitzenberger Steven M.,
McGaughey Georgia B.,
Colussi Dennis,
Lai MingTain,
Huang Qian,
Tugusheva Katherine,
Espeseth Amy S.,
Simon Adam J.,
Munshi Sanjeev K.,
Vacca Joseph P.
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700038
Subject(s) - chemistry , potency , combinatorial chemistry , drug , stereochemistry , amine gas treating , enzyme , pharmacology , drug discovery , protease inhibitor (pharmacology) , protease , biochemistry , in vitro , medicine , organic chemistry , family medicine , human immunodeficiency virus (hiv) , antiretroviral therapy , viral load
Structure‐based drug design was used to incorporate the traditional hydroxyethyl amine aspartyl protease inhibitor motif into 2,3,5‐substituted imidazolidin‐4‐one structures with good BACE‐1 enzyme inhibitory potency. These compounds represent a promising drug target for Alzheimer′s disease‐modifying therapy and are therefore of interest to the medicinal chemistry community.