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Page 1
Norbornadiene-dihydroazulene conjugates.
Kilde MD, Mansø M, Ree N, Petersen AU, Moth-Poulsen K, Mikkelsen KV, Nielsen MB. Kilde MD, et al. Org Biomol Chem. 2019 Sep 7;17(33):7735-7746. doi: 10.1039/c9ob01545k. Epub 2019 Aug 6. Org Biomol Chem. 2019. PMID: 31386755
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Kimura T, Shuto D, Hamada Y, Igawa N, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Kiso Y. Kimura T, et al. Bioorg Med Chem Lett. 2005 Jan 3;15(1):211-5. doi: 10.1016/j.bmcl.2004.09.090. Bioorg Med Chem Lett. 2005. PMID: 15582441
Recently, we reported potent and small-sized BACE1 inhibitors KMI-358 and KMI-370 in which the Glu residue is replaced by a beta-N-oxalyl-DAP (l-alpha,beta-diaminopropionyl) residue at the P(4) position. ...Hence, we used a tetrazole moiety as a bioisostere of the f …
Recently, we reported potent and small-sized BACE1 inhibitors KMI-358 and KMI-370 in which the Glu residue is replaced by a be …
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
Hamada Y, Igawa N, Ikari H, Ziora Z, Nguyen JT, Yamani A, Hidaka K, Kimura T, Saito K, Hayashi Y, Ebina M, Ishiura S, Kiso Y. Hamada Y, et al. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4354-9. doi: 10.1016/j.bmcl.2006.05.046. Epub 2006 Jun 6. Bioorg Med Chem Lett. 2006. PMID: 16757166
Recently, we reported potent and small-sized beta-secretase (BACE1) inhibitors KMI-570 and KMI-684 in which we replaced carboxylic acid groups at the P(1)(') position of KMI-420 and KMI-429, respectively, with tetrazole derivatives as carboxylic acid b …
Recently, we reported potent and small-sized beta-secretase (BACE1) inhibitors KMI-570 and KMI-684 in which we replaced carbox …
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Kimura T, Shuto D, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Hattori C, Asai M, Kitazume S, Saido TC, Ishiura S, Kiso Y. Kimura T, et al. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1527-31. doi: 10.1016/j.bmcl.2003.12.088. Bioorg Med Chem Lett. 2004. PMID: 15006396
Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE1 inhibitor KMI-370 (IC(50)=3. …
Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as …
38 results