- TARGETED DELIVERY TO BETA CELLS
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The disclosure includes zinc prodrugs for targeted delivery of therapeutic, diagnostic or imaging agents to β-cells and methods of use therefor. The disclosure also includes targeted delivery of small molecules to β-cells that stabilize and activate CRISP
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- Efficient synthesis of sivelestat sodium hydrate
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An efficient and scaleable synthesis of sivelestat sodium hydrate has been developed. Copyright Taylor & Francis Group, LLC.
- Bijukumar,Maloyesh,Sampat,Bhirud,Rajendra
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p. 1718 - 1724
(2008/09/20)
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- Application of the 'direct amide cyclization' to peptides containing an anthranilic acid residue
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The 2,2-disubstituted 2H-azirin-3-amines 7a-7c were used as amino acid synthons to prepare linear peptides derived from anthranilic acid. These linear peptides, which contain α,α-disubstituted α-amino acids, were synthesized by using the 'azirine/oxazolon
- Philipova, Irena,Linden, Anthony,Heimgartner, Heinz
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p. 1711 - 1733
(2007/10/03)
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- Neutral, acidic, and basic derivatives of anthranilamide that confer different formal charge to reducing oligosaccharides
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To facilitate the use of oligosaccharides as analytical tools in biological studies, we have designed, synthesized, and conjugated to maltosaccharides a novel series of homologous small fluorescent moieties that differ in formal charge. These moieties are
- Locke, Darren,Bevans, Carville G.,Wang, Lai-Xi,Zhang, Ye,Harris, Andrew L.,Lee, Yuan C.
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p. 221 - 231
(2007/10/03)
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- Synthesis and in Vitro Aldolase Reductase Inhibitory Activity of Compounds Containing an N-Acylglycine Moiety
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A number of N-benzoylglycines (6), N-acetyl-N-phenylglycines (7), N-benzoyl-N-phenylglycines (8), and tricyclic N-acetic acids (9-12) were synthesized as analogues of the N-acylglycine-containing aldolase reductase inhibitors alrestatin and 2-oxoquinoline-1-acetic acid.Derivatives of 6, which represent ring-simplified analogues of alrestatin, are very weak inhibitors of aldolase reductase obtained from rat lens, producing 50percent inhibition only at concentrations exceeding 100 μM.Compounds of series 7 were designed as ring-opened analogues of the 2-oxoquinolines.While this derivatives are more potent than compounds of series 6 (IC 50s of 6-80 μM), they are less active than the corresponding 2-oxoquinolines.Analogues of series 8 were designed as hybrid structures of both alrestatin and the 2-oxoquinoline-1-acetic acids.These compounds are substantially more potent than compounds of series 6 and 7 and display inhibitory activities comparable to or greater than alrestatin or the 2-oxoquinolines (IC 50s of 0.1-10 μM).Of the rigid analogues of 8, the most potent derivative is benzoxindol (12) with an IC 50 of 0.67 μM, suggesting that fusion of the two aromatic rings of 8 in a coplanar conformation may optimize affinity for aldose reductase in this series.
- DeRuiter, Jack,Swearingen, Blake E.,Wandrekar, Vinay,Mayfield, Charles A.
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p. 1033 - 1038
(2007/10/02)
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