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Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
A novel series of benzimidazoles was identified and optimized, leading to the discovery of potent and selective antagonists of the human melanocortin-4 receptor. In addition, compound 5i was shown toExpand
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Synthesis of azasugars as potent inhibitors of glycosidases.
A series of enantiomerically pure azasugars (2,5-dideoxy-2, 5-imino-D-mannitol, 1-deoxynojirimycin, 1-deoxymannojirimycin, and related compounds) was synthesized from D-mannitol viaExpand
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Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
Using a solution-phase parallel synthesis strategy, a series of non-peptide somatostatin analogues were prepared, and their binding affinities to the five human somatostatin receptor subtypesExpand
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Polyhydroxylated piperidines and azepanes from D-mannitol synthesis of 1-deoxynojirimycin and analogues
Abstract D -mannitol and L -iditol bis-epoxides, easily obtained from D -mannitol, are convenient substrates for the synthesis of polyhydroxylated piperidines and azepanes, via a nucleophilic openingExpand
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Synthesis of substituted imidazopyrazines as ligands for the human somatostatin receptor subtype 5.
A new preparation of trisubstituted imidazopyrazines and dihydroimidazopyrazines via parallel synthesis using aminoacids and bromoketones resulted in the discovery of non-peptidic sst5 selectiveExpand
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Design, synthesis and binding affinities of novel non-peptide mimics of somatostatin/sandostatin®
Abstract Based on molecular modelling studies of Sandostatin®, sugar-based derivatives I-VI were prepared as potential non-peptide mimics of somatostatin/Sandostatin®. These compounds displaced 3-[Expand
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Synthesis of azasugars. Part 2 isomerization of polyhydroxylated azepanes
Abstract Isomerization of enantiopure C2-symmetric 3,5-dihydroxyazepane derivatives has been studied. The neighboring nitrogen participation occurs during mesylation to give a chloromethylpiperidine,Expand
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Novel non-peptide ligands for the somatostatin sst3 receptor.
A series of imidazole derivatives has been prepared using high throughput parallel synthesis. Several compounds showed high affinity (Ki in 10(-6)-10(-8) M range) and selectivity at recombinant humanExpand
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Synthesis of azasugars. Part 1 isomerization of polyhydroxylated piperidines
Abstract N- Benzyl -3,4- di -O- benzyl-1,5-dideoxy-1,5-imino- d -glucitol and l -gulitol undergo easy isomerization, mainly either by ring contraction, or either by SN 2 inversion at C2. ThisExpand
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SYNTHESIS OF SUGAR-LIKE AMINO-CARBOXYLIC ACIDS FROM D-MANNITOL
Abstract 6-Amino-2,5-anhydro-6-deoxy- D -gluconic and L -gulonic acid derivatives, conformationally restricted sugar-like amino-carboxylic acids which mimic dipeptides, have been synthesized by aExpand
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