23516-80-5Relevant articles and documents
An improved synthesis of 3-[3-(trifluoromethyl)-3H-1,2-diazirin-3-yl]aniline: A key intermediate in the synthesis of photoaffinity probes
Wixe, Torbj?rn,Almqvist, Fredrik
, p. 3350 - 3352 (2017)
An improved synthesis of 3-[3-(trifluoromethyl)-3H-1,2-diazirin-3-yl]aniline, achieving an overall yield of 38% over seven steps is reported. Only three chromatographic separations were needed and the preparation of ~0.7?g of the target compound was demon
THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
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, (2013/07/19)
Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases
BACE1 inhibitors: Optimization by replacing the P1′ residue with non-acidic moiety
Hamada, Yoshio,Abdel-Rahman, Hamdy,Yamani, Abdellah,Nguyen, Jeffrey-Tri,Stochaj, Monika,Hidaka, Koushi,Kimura, Tooru,Hayashi, Yoshio,Saito, Kazuki,Ishiura, Shoichi,Kiso, Yoshiaki
, p. 1649 - 1653 (2008/12/22)
Recently, we reported potent BACE1 inhibitors KMI-429, -684, and -574 possessing a hydroxymethylcarbonyl isostere as a substrate transition-state mimic. These inhibitors showed potent inhibitory activities in enzymatic and cell assays, especially, KMI-429 was confirmed to significantly inhibit Aβ production in vivo. However, acidic moieties at the P4 and P1′ positions of KMI-compounds were thought to be unfavorable for membrane permeability across the blood-brain barrier. Herein, we replaced acidic moieties at the P4 position with other hydrogen bond acceptor groups, and these inhibitors exhibited improved BACE1 inhibitory activities in cultured cells. In this study, we replaced the acidic moieties at the P1′ position with non-acidic and low molecular sized moieties.