210530-70-4Relevant articles and documents
Pyrrolidone derivative
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Paragraph 0146; 0150-0151, (2021/03/13)
The present invention relates to a pyrrolidone derivative and a pharmaceutically acceptable composition thereof, which are useful as inhibitors of methionine aminopeptidase.
SGC STIMULATORS
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Page/Page column 00262, (2018/05/27)
The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an inc
Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design
Hamada, Yoshio,Tagad, Harichandra D.,Nishimura, Yoshinori,Ishiura, Shoichi,Kiso, Yoshiaki
scheme or table, p. 1130 - 1135 (2012/03/26)
Previously reported pentapeptidic BACE1 inhibitors, designed using a substrate-based approach, were used as lead compounds for the further design of non-peptidic BACE1 inhibitors. Although these peptidic and non-peptidic inhibitors, with a hydroxymethylcarbonyl isostere as a substrate transition-state mimic, exhibited potent BACE1 inhibitory activities, their molecular-sizes appeared a little too big (molecular weight of >600 daltons) for developing practical anti-Alzheimer's disease drugs. To develop lower weight BACE1 inhibitors, a series of tripeptidic BACE1 inhibitors were devised using a design approach based on the conformation of a virtual inhibitor bound to the BACE1 active site, also called 'in-silico conformational structure-based design'. Although these tripeptidic BACE1 inhibitors contained some natural amino acid residues, they are expected to be useful as lead compounds for developing the next generation BACE1 inhibitors, due to their low molecular size and unique structural features compared with previously reported inhibitors.