- Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.
Bioorganic & medicinal chemistry letters (2008-04-25)
Heuisul Park, Kyeongsik Min, Hyo-Shin Kwak, Ki Dong Koo, Dongchul Lim, Sang-Won Seo, Jae-Ung Choi, Bettina Platt, Deog-Young Choi
PMID18434152
ZUSAMMENFASSUNG
We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2' and combination of SAR display a >100-fold increase in potency with good cellular activity (IC(50)=0.15microM) relative to the previously reported compound 3.
MATERIALIEN