• 대한의용생체공학회:의공학회지
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• 제15권1호
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• pp.89-96
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• 1994

키틴의 글루코사민 단위에 클로로프로판, 산화프로필렌 그리고 클로로프로판 디올을 반응시켜 프로필 키틴(PPC), 히드록시프로필 키틴(HPC), 디히드록시프로필 키틴(DHPC)등의 에테르 형태의 키틴 유도체를 합성하였고, 이들을 99% 포름산에 용해시켜 고분자 농도 30 wt%이상에서 콜레스테릭한 유방성 액정을 형성하였다. 액정이 형성된 용액으로부터 필름을 제조하여 라이소자임이 포함된 유사 체액, pH 1.2, pH 6.7 그리고 pH 8.2 용액에서 in vitro 분해정도를 관찰한 결과 처음 1주일에서 급격하게 분해되었으며 중성 영역에서 큰 무게 감소와 기계적 강도가 감소하였다. 세가지 시료들 중 DHPC가 가장 좋은 생분해 정도를 나타냈다.

• 약학회지
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• 제35권1호
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• pp.7-10
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• 1991

For the purpose of developing of anticariogenic agents, P-phenylphenol derivatives were synthesized and determined their antibacterial activities against a cariogenic bacterium, Streptococcus mutans. Among synthetic compounds, 2-nitro-6-bromo-p-phenylphenol showed as potent antibacterial activity as magnolol and honokiol.

• Archives of Pharmacal Research
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• 제17권2호
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• pp.119-123
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• 1994

The synthesis of 3a, 3b, 7a fro Benzpthiazepinone and 1,4-dihyropyridine derivatives is described. Benzothiazepinone nad 1,4-dihydropyridine derivatives were prepared according to literature procedure. The key reactions involve esterification and amidation of benzothize-pinone nad 1,4-dihydropyridine derivatives.

• Bulletin of the Korean Chemical Society
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• 제17권4호
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• pp.314-321
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• 1996

Isoxazolidine derivatives 7 and 8 were synthesized from N-benzyl-C-(2-benzyloxyethyl)nitrones by 1,3-dipolar cycloaddition with ethyl crotonate. The isoxazolidine derivatives were converted to β-amino acid esters 9a and 9b by reduction with zinc in acetic acid. The β-amino acid esters were reacted with methylmagnesium bromide to give the 2-azetidinones (13a, 13b). The benzyl group of 2-azetidinones were removed by Birch reduction. The products were oxidized with PDC to give 3-[1-(t-butyldimethylsilyloxy)ethyl]-4-carboxymethyl-2-azetidinone derivatives (2a, 2c).

• Archives of Pharmacal Research
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• 제17권6호
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• pp.483-486
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• 1994

A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, C glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)amino]-7-chloro-5, 8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5, and 7 showed more potent antifungal activities than kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

• Bulletin of the Korean Chemical Society
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• 제31권7호
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• pp.1837-1838
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• 2010

• 약학회지
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• 제58권1호
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• pp.21-27
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• 2014

We have developed 8 peptide derivatives as potential MC1R antagonists and their inhibitory effects on ${\alpha}$-MSH induced cell growth in cultured normal human melanocytes (NHM) were investigated. From these experiments, the two most potent peptide derivatives, 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_6NH_2$ (P 6) and 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_9NH_2$ (P 7) were selected for further studies. In ${\alpha}$-MSH depleted NHM cells, we have found that the treatment with 1 ${\mu}M$ of these two peptide derivatives, P 6 and P 7, inhibited the cell proliferation induced by the addition of 1 nM ${\alpha}$- MSH by 70% and 72%, respectively. In NHM cells without previous ${\alpha}$-MSH depletion, 1 ${\mu}M$ treatment in the presence of 10 nM ${\alpha}$-MSH resulted in 70% (P 6) and 80% (P 7) decrease in cell growth and 64% (P 6) and 71% (P 7) reduction in melanin synthesis, respectively. The peptide derivatives P 6 and P 7 were proved to have no apparent cytotoxicity and inhibited the elevation of intracellular cAMP concentration triggered by ${\alpha}$-MSH. In conclusion, our data suggest that the peptide derivatives reported in this study, 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_6NH_2$ (P 6) and 5-phenylvaleric acid-(D)His- Arg-Trp-$(Lys)_9NH_2$ (P 7) strongly antagonize ${\alpha}$-MSH, inhibit cell proliferation and melanin synthesis, and lower the intracellular cAMP concentration, hence have a promising potential as a novel skin lightening agent.

• 대한화학회지
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• 제64권1호
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• pp.7-18
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• 2020

An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, ¹H NMR, ¹³C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

• Bulletin of the Korean Chemical Society
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• 제34권7호
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• pp.2111-2116
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• 2013

This paper reports substituent effects on the conformational changes in polyaniline (PAni) derivatives. PAni, poly-o-toluidine (POT), and poly-o-anisidine (POA) were formed by potentiodynamic electropolymerization in aqueous solution containing (+)-camphorsulfonic acid (CSA) as a dopant. UV-Vis spectroscopy and cyclic voltammetry measurements revealed that the methyl group showed a greater steric hindrance than the methoxy group. Further, the doping level decreased with increasing steric hindrance. The sign pattern of the circular dichroism (CD) bands for POA was opposite to that for PAni. However, no CD bands were observed in POT. The steric hindrance caused helical inversion, but at a high level of steric hindrance, the helical conformation could not be adopted, because of the reduced doping level. The reduced crystallinity was greatly affected by the decreased doping level. The steric effect influenced the polymer conformation and the doping level, thus determining the optical activity, morphology, and crystallinity of the PAni derivatives.

• 대한화학회지
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• 제25권3호
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• pp.199-205
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• 1981

Aniline과 alcohol류에서 4-aminoalkylbenzene을 合性하여, 이것을 아세틸化, 니트로化, 加水分解하여 3-nitro-4-aminoalkylbenzene을 얻고 아미노기 이탈반응을 통해 3-nitroalkylbenzene을 合成하여 anthranilic acid와 반응시켜 7-alkyl-1-carboxyphenazine 유도체를 合成하였다. 生成物은 元素分析, IR, NMR 스펙트럼으로 確認하였다. 이들 誘導體들의 水溶液에 대한 表面張力을 測定하였고, 아울러 Gram 陽性菌, Gram 陰性菌, 眞性菌에 대한 抗菌性을 調査하였다. 試驗結果 alkyl기가 치환된 phenazine 誘導體의 抗菌性은 alkyl기가 없는 1-carboxyphenazine 보다 强한 것으로 나타났다.