Abstract
Thiol-thioester exchange was found to readily generate libraries of cyclic thiodepsipeptides under thermodynamic control, which will enable their use in a variety of dynamic combinatorial chemistry assays. The kinetic determinants of macrocycle formation and the role of amino acid structure on the r...
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PMID: 20329734
PDF is available here.
Abstract
In this work, a sandwich monoclonal-based ELISA for quantifying the HBsAg obtained from yeast cells was standardized and validated. The monoclonal antibody employed in this assay reacts uniformly with different molecular isoforms of r-HBsAg. Immunoassay allowed the r-HBsAg quantification in an analy...
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PMID: 20188925
PDF is available here.
Abstract
We demonstrate how a combination of enabling technologies such as flow synthesis, solid-supported reagents and scavenging resins utilised under fully automated software control can assist in typical medicinal chemistry programmes. In particular automated continuous flow methods have greatly assisted...
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PMID: 20449482
PDF is available here.
Abstract
Of the thousands of known chemical reactions, a handful of reactions, called "click" reactions, stand out with features such as good chemoselectivity, good solvent compatibilities, modularity, minimum synthetic demands, bioorthogonality and high yields. Among them, the Cu(i)-catalyzed 1,3-dipolar cy...
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PMID: 20449474
PDF is available here.
Abstract
The reaction of 2-aminoaryl ketones and arynes generated by the treatment of various o-(trimethylsilyl)aryl triflates with CsF results in [4 + 2] annulation to afford substituted acridines in good yields.
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PMID: 20222700
PDF is available here.
Abstract
The synthesis of a series of substituted phenanthridines by photostimulated C-C cyclization of anions from N-(ortho-halobenzyl)arylamines has been found to proceed in very good to excellent yields (79-95%) in liquid ammonia and in DMSO. The N-(ortho-halobenzyl)arylamines are obtained in good to very...
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PMID: 20210329
PDF is available here.
Abstract
An efficient method for the synthesis of symmetrical and unsymmetrical substituted thiourea derivatives by means of simple condensation between available building blocks such as amines and carbon disulfide in aqueous medium is presented. This protocol works smoothly with aliphatic primary amines to...
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PMID: 20201494
PDF is available here.
Abstract
The first synthesis of the marine endoperoxide 9,10-dihydroplakortin, of its C10-desethyl analogue, and of their corresponding C6 epimers is described. Stereogenic centers at C4 and at the lateral chain have been stereoselectively synthesized through Evans' chiral auxiliary chemistry. Moreover, the...
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PMID: 20199093
PDF is available here.
Abstract
A mild and efficient method for the synthesis gamma-DDB has been developed through anhydride-linker assisted intramolecular Ullmann reaction. Highly regioselective bromination of differentially protected gallate was realized by virtue of the introduction of NBS.
2010 Elsevier Ltd. All rights reserve...
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PMID: 20207147
PDF is available here.
Abstract
We will discuss several concepts of combinatorial libraries and provide information as what to expect from these depending on the given context....
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PMID: 20428057
PDF is available here.
Abstract
The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from beta-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. Th...
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PMID: 20428042
PDF is available here.
Abstract
Nanoliter plates are versatile tools for the screening of split-and-mix libraries both on-bead and off-bead. The method was evaluated for the identification of hydrolytically active compounds and enzyme inhibitors.
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PMID: 20234908
PDF is available here.
Abstract
We report herein an expressed peptide assay scheme, by using nanoparticle probes, for detecting DNA hybridization events. The method exploits plasmid-encoded peptide tags as surrogate molecules for the matrix-assisted laser desorption/ionization time-of-flight mass spectrometry identification of tar...
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PMID: 20210312
PDF is available here.
Abstract
We report here two self-replicating peptide-derived macrocycles that emerge from a small dynamic combinatorial library and compete for a common feedstock. Replication is driven by nanostructure formation, resulting from the assembly of the peptides into fibers held together by beta sheets. Which of...
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PMID: 20299594
PDF is available here.
Abstract
We describe the method for high-throughput screening and profiling of metalloproteases on small molecule microarrays. Metalloproteases are an important class of proteins, which are implicated in the pathogenicity of certain microbes and in the progression of cancer. We have introduced a novel two-co...
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PMID: 20217580
PDF is available here.
Abstract
We find that the polymerization sequence most affects hydrogen bonding and aromatic ring bond energies. This work defines the relationships between chemistry, structure, processing, and properties of the IPN samples....
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PMID: 20030378
PDF is available here.
Abstract
We present a strategy that facilitates the development of MRM assays for large numbers of unpurified low-abundance proteins. Our discovery strategy is based on the reduction of the dynamic range of protein concentrations in biological fluids by means of one-bead one-compound combinatorial peptide li...
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PMID: 20070123
PDF is available here.
Abstract
The introduction of different methodologies for the construction and screening of complex protein libraries has provided powerful means in protein engineering for the development of molecules with desired traits. A challenge faced in many situations is to adapt a given methodology for efficient and...
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PMID: 20121700
PDF is available here.
Abstract
Synthesis and evaluation of anti-TB activity of individual compounds of Schiff bases combinatorial library were done against Mycobacterium tuberculosis H(37)Rv at a single concentration of 6.25mug/mL according to the protocol of TAACF. Compounds 2C and 3D produced 99% inhibitory activity on the inve...
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PMID: 20045582
PDF is available here.
Abstract
We have used computer-assisted combinatorial techniques to design, focus using the NS2B-NS3pro receptor 3D structure, and in silico screen a virtual library of more than 9,200 peptidomimetic analogs targeted around the template inhibitor Bz-Nle-Lys-Arg-Arg-H (Bz-benzoyl) that are composed mainly of...
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PMID: 20306283
PDF is available here.
Abstract
An efficient and simple two-step procedure for the formation of hydroxy-Freidinger lactams is presented. The methodology allows assembly of the cyclic threonine motif (cThr) in solution and on solid support during conventional peptide synthesis.
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PMID: 20449272
PDF is available here.
Abstract
I will also briefly review some recent uses of the technology to illustrate its incredible versatility....
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PMID: 20196239
PDF is available here.
Abstract
Highly enantio- and diastereoselective organocatalytic Mannich reactions of glycine Schiff bases with N-Boc-protected imines are described. Imines were generated in situ from bench-stable alpha-amido sulfones. Catalysis mediated by a cinchona alkaloid thiourea provided optically acti...
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PMID: 20085291
PDF is available here.