Application Of Combinatorial Chemistry Research Articles

New multi-coupling benzylic zinc reagents for the preparation of flexible aromatic compounds

The benzylic zinc reagents 3a-c bearing a triflate group in o-, m- or p-position are new efficient multi-coupling reagents reacting stepwise with an aryl iodide (Ar 1I) and an arylzinc bromide (Ar 2ZnBr) in the presence of the appropriate palladium catalyst and the suitable phosphine ligand leading to polyfunctional flexible aromatic products of type 5. This methodology is appropriate for applications in combinatorial chemistry.

Drug-motif-based diverse monomer selection: Method and application in combinatorial chemistry

This article describes a strategy to explore monomer diversity while incorporating drug motif knowledge into the design and selection of monomers for combinatorial chemistry. The process involves collecting from available electronic databases all those molecules that potentially could be monomers. In this manner we have assembled five DAYLIGHT databases, each containing one of the common functional groups: carboxylic acids, aldehydes, nitriles, primary amines, and secondary amines. The molecules in the databases are then subjected to fingerprint and cluster analysis using the Jarvis-Patrick algorithm and profiles of the compounds are calculated relating to molecular weight, H-bond counts, and rotatable bond flexibility. The cluster information and profiles of the molecules are stored back into the databases for similarity and diversity searches, and for profile prescreening of monomers. To apply drug motif knowledge to a selection an application to an aldehyde set is discussed, in which representatives of each cluster in the aldehyde database are compared with drug molecules in the Standard Derwent File (SDF) in one of three ways to select drug motif-based monomers for purchase or synthesis.

ChemInform Abstract: Solid Phase Synthesis of Aryl and Benzylpiperazines and Their Application in Combinatorial Chemistry.

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Protein Kinase C: Structure, Function, and Regulation

The protein kinase C family of enzymes transduces the myriad of signals promoting lipid hydrolysis. The prevalence of this enzyme family in signaling is exemplified by the diverse transduction mechanisms that result in the generation of protein kinase C's activator, diacylglycerol. Signals that stimulate members of the large families of G protein-coupled receptors, tyrosine kinase receptors, or non-receptor tyrosine kinases can cause diacylglycerol production, either rapidly by activation of specific phospholipase Cs or more slowly by activation of phospholipase D to yield phosphatidic acid and then diacylglycerol(1, 2, 3) . In addition, fatty acid generation by phospholipase A2 activation modulates protein kinase C activity(3) . Thus, multiple receptor pathways feeding into multiple lipid pathways have the common end result of activating protein kinase C by production of its second messenger.

Solid Phase Synthesis of Aryl and Benzylpiperazines and their Application in Combinatorial Chemistry

Solid Phase Synthesis of Aryl and Benzylpiperazines and their Application in Combinatorial Chemistry

Solid phase synthesis of aryl and benzylpiperazines and their application in combinatorial chemistry

An S NAr reaction on solid phase was demonstrated in the synthesis of a piperazine library using a combinatorial approach.