6659-35-4Relevant articles and documents
Discovery and initial optimization of 5,5′-disubstituted aminohydantoins as potent β-secretase (BACE1) inhibitors
Nowak, Pawel,Cole, Derek C.,Aulabaugh, Ann,Bard, Jonathan,Chopra, Rajiv,Cowling, Rebecca,Fan, Kristi Y.,Hu, Baihua,Jacobsen, Steve,Jani, Minakshi,Jin, Guixan,Lo, Mei-Chu,Malamas, Michael S.,Manas, Eric S.,Narasimhan, Rani,Reinhart, Peter,Robichaud, Albert J.,Stock, Joseph R.,Subrath, Joan,Svenson, Kristine,Turner, Jim,Wagner, Erik,Zhou, Ping,Ellingboe, John W.
scheme or table, p. 632 - 635 (2010/06/12)
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine (1) was identified through HTS, as a weak (micromolar) inhibitor of BACE1. X-Ray crystallographic studies indicate the 2-aminoimidazole ring forms key H-bonding interactions with Asp32 and Asp228 in the catalytic site of BACE1. Lead optimization using structure-based focused libraries led to the identification of low nanomolar BACE1 inhibitors such as 20b with substituents which extend from the S1 to the S3 pocket.
Mass labels
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, (2008/06/13)
Provided is a set of two or more mass labels, each label in the set comprising a mass marker moiety attached via a cleavable linker having at least one amide bond to a mass normalisation moiety, wherein the aggregate mass of each label in the set may be the same or different and the mass of the mass marker moiety of each label in the set may be the same or different, and wherein in any group of labels within the set having a mass marker moiety of a common mass each label has an aggregate mass different from all other labels in that group, and wherein in any group of labels within the set having a common aggregate mass each label has a mass marker moiety having a mass different from that of all other mass marker moieties in that group, such that all of the mass labels in the set are distinguishable from each other by mass spectromety, and wherein the mass marker moiety comprises an amino acid and the mass normalisation moiety comprises an amino acid.
Wrinkle-care product
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, (2008/06/13)
A wrinkle-care product, an aging-preventive cosmetic and a skin cosmetic each comprising a guanidine derivative of formula (I) or an acid addition salt thereof: STR1 wherein R1 represents a hydrogen atom, a lower alkyl group or --(AO)m --(BO)n --D--E ?wherein A and B may be the same or different and each represents an alkylene group having 2 to 8 carbon atoms; D represents a binding hand, --CO--, or an unsubstituted or substituted alkylene group having 1 to 6 carbon atoms; E represents a hydrogen atom, a lower alkyl group, an aralkyl group or an unsubstituted or substituted aryl group; m is a number of from 1 to 6; and n is a number of from 0 to 6!; k is a number of from 1 to 10; and G represents a hydrogen atom, a hydroxyl group, a carboxyl group, a sulfonate group or a phosphate group. These products are excellent in the effects of inhibiting wrinkling and smoothing wrinkles without damaging the physiological conditions of the skin.