• Archives of Pharmacal Research
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• 제25권6호
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• pp.801-806
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• 2002

Cyclicpeptides are important targets in peptide synthesis because of their interesting biological properties. Constraining highly flexible linear peptides by cyclization is one of the mostly widely used approaches to define the bioactive conformation of peptides. Cyclic peptides often have increased receptor affinity and metabolic stability over their linear counterparts. We carried out virtual screening experiment via docking in order to understand the interaction between HLE-Human Leukocyte Elastase and ligand peptide and to identify the sequence that can be a target in various ligand peptides. We made cyclic peptides as a target base on Metlle-Phe sequence having affinity for ligand and receptor active site docking. There are three ways to cyclize certain sequences of amino acids such as Met-lie-Phe-Gly-Ile. First is head-to-tail cyclization method, linking between N-terminal and C-terminal. Second method utilizes amino acid side chain such as thiol functional group in Cys, making a thioether bond. The last one includes an application of resin-substituted amino acids in solid phase reaction. Among the three methods, solid phase reaction showed the greatest yield. Macrocyclization of Fmoc-Met-Ile-Phe-Gly-Ile-OBn after cleavage of Fmoc protection in solution phase was carried out to give macrocyclic compound 5 in about 7% yield. In the contrast with solution phase reaction, solid phase reaction for macrocyclization of Met-Ile-Phe-Gly-Ile-Asp-Tentagel in normal concentrated condition gave macrocyclic compound 7 in more than 35% yield.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.75-76
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.159.2-159.2
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.214.1-214.1
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.246.1-246.1
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• 2003

Hetero chain compounds have high possibilities of being good medicinal candidate because of their well-known medicinal activity and relatively low subtitled carbon. By constructing the method of making this compound library, this research has the purpose to create a new medicinal candidate materials based on an easy medicinal search. The first step is to construct an Indole library in a compounding process with the design of a linker connecting a solid-state resin and a substrate. (omitted)

• 대한화학회지
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• 제44권1호
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• pp.30-36
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• 2000

A-factor,(3R)-2-(6-methylheptanoyl)-3-hydroxymethyl-4-butanolide(1)의 전합성을 위하여 선택된 중간체, (2R)-2-(N,N-ditosylimido)-3-butenyl methyl malonate(4)의 Pd(0) 촉매 커플링 반응에서 예상과는 다르게 14각 고리화합물인 bis(2-methoxycarbonyl-(4E)-hexenolide)(15)가 생성되었다. 이 화합물은 X-ray 결정학을 이용하여 구조를 확인하였다. 이 결과는 다양한 크기의 대칭적인 거대고리화합물을 합성할 수 있다는 것을 제시해 주고 있다.