130333-58-3Relevant academic research and scientific papers
NOVEL FLUORESCENT DYES AND USES THEREOF
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Page/Page column 45, (2011/02/24)
The present invention provides fluorescent dyes that are based on firefly luciferin structure. These dyes are optimally excited at shorter wavelengths and have Stokes shift of at least 50 nm. The fluorescent dyes of the invention are useful for preparation of dye-conjugates, which can be used in detection of an analyte in a sample.
N-[1-(3-AMINO-4-PHENYL-BUTYRYL)-4-HYDROXY-PYRROLIDIN-2-YLMETHYL}-PROPIONAMIDE AND RELATED COMPOUNDS AS DPP-IV INHIBITORS FOR THE TREATMENT OF TYPE 2 DIABETES MELLITUS
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Page/Page column 55, (2010/11/30)
The invention relates to compounds of formula (I) and formula (II) wherein Z1 R1-5, R, W, X, Y, m, n and A1 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention al
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Page/Page column 74, (2010/11/27)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
Desazadesmethyldesferrithiocin analogues as orally effective iron chelators
Bergeron, Raymond J.,Wiegand, Jan,Weimar, William R.,Vinson, J. R. Timothy,Bussenius, J?rg,Yao, Guo Wei,McManis, James S.
, p. 95 - 108 (2007/10/03)
Further structure-activity studies of desferrithiocin analogues are carried out. (S)-Desazadesmethyldesferrithiocin, 2-(2-hydroxyphenyl)-Δ2- thiazoline-4(S)-carboxylic acid, serves as the principal framework in the current paper. Desazadesmethyldesferrithiocin can be structurally altered with facility, and data are already available on its iron-clearing properties and toxicity parameters. Four different kinds of structural modifications of this framework are undertaken: introduction of hydroxy, carboxy, or methoxy groups on the aromatic ring; alteration of the thiazoline ring; increasing the distance between the ligand donor atoms; and benz-fusion of the aromatic rings. The structural modifications described are shown to have a tremendous impact on both the iron clearance and toxicity profiles of the desazadesmethyldesferrithiocin molecule. All of the compounds are assessed in a bile-duct-cannulated rodent model to determine iron clearance efficiency. Ligands which demonstrate an efficiency of greater than 2% are carried forward to the iron-overloaded primate for iron-clearing measurements. Ligands with efficiencies greater than 3% in the primate are then evaluated in a formal toxicity study in rodents. On the basis of the results of the present work, 2-(2,4-dihydroxyphenyl)-Δ2-thiazoline-4(S)-carboxylic acid is a promising candidate for clinical evaluation.
Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors
Chauvel,Coric,Llorens-Cortes,Wilk,Roques,Fournie- Zaluski
, p. 1339 - 1346 (2007/10/02)
Aminopeptidase A (APA) and aminopeptidase N (APN) are two metallopeptidases which have been suggested to be involved in the enzymatic cascade of the renin-angiotensin system. APA liberates angotensin III from angiotensin II by releasing the N-terminal asp
Chirospecific synthesis of amino acids, amino aldehydes and amino alcohols from D-glucosamine hydrochloride. A multigram synthesis of N-BOC-L-serinal
Giannis,Henk
, p. 1253 - 1256 (2007/10/02)
N-tert.-butyloxycarbonyl-L-serinal 4 was readily prepared from D-glucosamine hydrochloride 1 in three steps. The versatile synthetic intermediate 4 is chemically and configurationally stable for prolonged time and reacts with various stabilized phosphorus
