• BMB Reports
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• v.38 no.5
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• pp.517-525
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• 2005

Solid phase peptide synthesis method, which was introduced by Merrifield in 1963, has spawned the concept of combinatorial chemistry. In this review, we summarize the present technologies of solid phase peptide synthesis (SPPS) that are related to combinatorial chemistry. The conventional methods of peptide library synthesis on polymer support are parallel synthesis, split and mix synthesis and reagent mixture synthesis. Combining surface chemistry with the recent technology of microelectronic semiconductor fabrication system, the peptide microarray synthesis methods on a planar solid support are developed, which leads to spatially addressable peptide library. There are two kinds of peptide microarray synthesis methodologies: pre-synthesized peptide immobilization onto a glass or membrane substrate and in situ peptide synthesis by a photolithography or the SPOT method. This review also discusses the application of peptide libraries for high-throughput bioassays, for example, peptide ligand screening for antibody or cell signaling, enzyme substrate and inhibitor screening as well as other applications.

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.811-815
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• 2004

Coumarin and its derivatives occur widely in nature. Many attempts were made for synthesis of various coumarin derivatives because of their interesting biological activities. In this study, solid phase synthetic approach of 3-(4-hydroxyphenyl)coumarin was achieved for combinatorial synthesis of substituted 3-phenylcoumarin analogues. Starting from 4-hydroxyphenylacetic acid methyl ester, release of 3-(4-hydroxypnehyl)coumarin from polymer support was accom-plished.

• Archives of Pharmacal Research
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• v.21 no.3
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• pp.330-337
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• 1998

N-(tert-Butoxycarbonyl)-O-(dimethythiophosphono)-L-tyrosine (6) and N-(tert-butoxycarbonyl)-O-(dicyanoethylthiophosphono)-L-tyrosine (15) were prepared as intermediates for the synthesis of thiophosphotyrosine-containing peptides. The reactivity and suitability of two compounds for the solid phase or solution phase peptide synthesis utilizing t-Boc chemistry were examined.

• Journal of the Institute of Electronics and Information Engineers
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• v.50 no.12
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• pp.184-190
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• 2013

Parametric stereo(PS) audio coding is a specific version of spatial audio coding. In this paper, the problem due to the conventional synthesis of phase differences. In the conventional upmix matrix, phase differences are synthesized not only on downmix signal but also ambient signal, which violates the assumption that the ambient signals are anti-phased. Deterioration due to the phase synthesis is analyzed, especially, for low interchannel correlation. To solve this problem, new upmix matrix is proposed, which synthesizes phase differences only on downmix signal. The performance of the proposed upmix matrix is verified by the subjective listening tests.

• Tribology and Lubricants
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• v.25 no.1
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• pp.7-12
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• 2009

Coating brittle intermetallic compounds on metal can enlarge the range of their use. It is found that intermetallic compound coating layers made by only combustion synthesis in an electric furnace have porous multi-phase structures containing several intermediate phases, even though the coating layers show good wear resistance. In this study, dense $Ni_{3}Al$ single phase layer corresponding to the initial composition of the mixed powder is coated on two different ferrous materials by the diffusing treatment after combustion synthesis. After- ward, sliding wear behaviors of the coating layer are evaluated in comparison with that of the coating layer with porous multi-phase structure made by only combustion synthesis. As a result, the wear properties of the coating layer composed of dense $Ni_{3}Al$ single phase are considerably improved at the range of low sliding speed com- pared with that of the coating layer with porous multi-phase structure, particularly in the running-in wear region. This is attributed to the fact that wear of the coating layer is progressed by shearing as a sequence of adhesion, not by occurring of pitting on the worn surface due to having dense structure without pores.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.25-30
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• 2004

Combinatorial homoserine lactone mixtures and individual products were obtained from the methionine-functionalized resin in solid-phase synthesis. The four-step process consisting of a coupling step of an N-Fmoc-L-methionine, deprotection of N-Fmoc group, N-coupling with a carboxylic acid, and cleavage reaction through a polymer supported strategy is described. Gas chromatography-mass selective detector (GC-MSD) techniques provide the most powerful methods for identifying both the combinatorial mixtures and individual products.

• Bulletin of the Korean Chemical Society
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• v.10 no.1
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• pp.19-22
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• 1989

The suitability of BMPI (2-bromo-N-methyl pyridinium iodide) for solid-phase peptide synthesis was investigated. The coupling rate of BMPI/HOBT procedure. BMPI/HOBT was superior to DCC/HOBT couplings using the solid-phase peptide bond formation proceeded to a greater degree of completion than DCC/HOBT method did. Double couplings with 2 equiv. of Bocamino acids and 1.5 equiv. of BMPI and $NEt_3$ and 2 equiv. of HOBT in DMF/MC (1:1 v/v) gave the best result for the preparation of a model compound. Stepwise solid phase peptide synthesis using BMPI/HOBT procedure was successfully utilized for the preparation of $(D-Ala)^2$-dynorphine A. BMPI/HOBT procedure for the synthesis of $(D-Ala)^2$-dynorphine gave better yield (20%) than DCC/HOBT procedure did.

• Bulletin of the Korean Chemical Society
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• v.24 no.3
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• pp.389-392
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• 2003

• Bulletin of the Korean Chemical Society
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• v.30 no.6
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• pp.1325-1330
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• 2009

A general method has been developed for the solid phase synthesis of drug-like 7-aryl-benzo[b][1,4]oxazin-3(4H)- one derivatives 6. The method relies on a novel, microwave irradiation promoted cyclization reaction of the BOMBA resin bound, N-substituted-$\alpha$-(2-chloro-4-bromophenoxy)acetamide 3 that takes place via a Smiles rearrangement. The 7-bromobenzo[1,4]oxazine 4, produced in this process is converted to 7-aryloxazin analogs 5 by utilizing Suzuki coupling with various substituted arylboronic acids. Finally, the target 7-aryl-benzo[b][1,4]oxazin-3(4H)-ones 6 are liberated from the resin by treatment with 5% TFA. The progress of the reactions involved in this preparative route can be monitored by using ATR-FTIR spectroscopy on a single bead. The target compounds, obtained by using this five-step sequence, are produced in high yields and purities.

• Bulletin of the Korean Chemical Society
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• v.23 no.11
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• pp.1658-1660
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• 2002