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P3‐001: Alzheimer's disease with and without vascular lesions
Author(s) -
Faqih Souhad Al
Publication year - 2008
Publication title -
alzheimer's and dementia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 6.713
H-Index - 118
eISSN - 1552-5279
pISSN - 1552-5260
DOI - 10.1016/j.jalz.2008.05.1564
Subject(s) - pathology , cerebral amyloid angiopathy , medicine , senile plaques , pathological , leukoaraiosis , lesion , white matter , hippocampal sclerosis , atrophy , angiopathy , vascular dementia , hyperintensity , dementia , alzheimer's disease , temporal lobe , disease , magnetic resonance imaging , radiology , diabetes mellitus , psychiatry , epilepsy , endocrinology
to the inhibitor structure, as well as filling extra binding pockets with additional functional groups. The optimised lead was shown to have enhanced activity with an IC50 towards BACE1 of 37 M. Analogues with IC50 100 M towards BACE1 were tested in the cellular assay, and selected compounds have shown promising cellular activity with EC50 10 M. Conclusions: The rational design approach using de novo design software SPROUT has successfully delivered a new cellular active BACE1 inhibitor scaffold.