• Title/Summary/Keyword: derivative synthesis

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Synthesis of Pyrazinopsoralen : A Pyrazine Ring Fused Monofunctional Psoralen Derivative

  • 유동진;전영희;김동원;한규석;심상철
    • Bulletin of the Korean Chemical Society
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    • v.16 no.12
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    • pp.1212-1218
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    • 1995
  • An efficient synthesis of 6,8-dioxa-1,4-diazacyclopenta[b]phenanthren-5-one (Pyrazinopsoralen) (4) has been carried out by the Suzuki coupling reaction as a key step starting from 5-bromo-6-methoxybenzofuran (6) and methyl 2-iodo-3-pyrazinecarboxylate (8).

The Synthesis of Kyotorphin Derivative by $\alpha$-Chymotrypsin ($\alpha$-Chymotrypsin 을 이용한 Kyotorphin 유도체의 합성)

  • Jeon, Yu Jin;Kim, Se Gwon
    • Journal of the Korean Chemical Society
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    • v.38 no.6
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    • pp.449-455
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    • 1994
  • In order to obtain the basic data for synthetic studies of bioactive peptide using enzyme, Kyotorphin(analgesic peptide) derivative was synthesized from Ac-Tyr-OH and $Arg-NH_2$ by $\alpha-chymotrysin$ in two phase system(organic phase and aqueous phase). In effect of organic solvent on Kyotorphin derivative synthesis from Ac-Tyr-OH(10 mM) and $Arg-NH_2$ (20 mM), the synthesis in ethyl acetate system of organic solvents was higher than those in other organic solvents (n-butanol, n-hexane, dichloromethane and chloroform). The optimal conditions for the synthesis are as follows: enzyme conc., 10 ${\mu}M;$ reaction pH, 7.0; reaction temp., $35^{\circ}C$ ; the ratio of organic phase volume/aqueous phase volume $(\alpha)$, 15. Under the optimal conditions, the yield was 70.2%, and the reaction achieved to equilibrium after 24 hrs.

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Synthesis and antitubercular activity of the nitrogen substituents of carbonylthicureas and carbonylthiosemicarbazides (Carbonyl thiourea 및 carbonyl thiosemicarbazide의 질소치환화합물의 합성 및 항결핵작용에 관한 연구)

  • 이남복
    • YAKHAK HOEJI
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    • v.17 no.4
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    • pp.223-234
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    • 1973
  • Sixteen compounds of N-aroyl-N'-(4'-alkoxyphenyl) thiourea derivative, twenty one compounds of N-aeryl-N'(3'-hydroxy-4'-alkoxycar-bonylphenyl) thiourea derivative, three compounds of N-aeroyl-N'-.alpha.-naphthyiourea derivative and three compounds of N-cyanoacetyl-N'-aroyl thiosemicarbazide derivative were syntrhesized as potential antitubercular agent and were subjected to screening test for antitubercular activity against Mycobacterium turberculosis H/sub 37/Rv by tube dilution method in vitro. Of the fourty three eompounds, N-p-cyanobenzoyl-N'-(4'-iso-butoxyphenyl) thiourea, N-p-cyanobenzoyl-N'-(4-n-amoxyphenyl)thiourea, N-furoyl-N'-(3'-hydroxy-4'-ethoxycarbonylphenyl)thiourea, N-p-cyanobenzoyl-N'-(3'-hydroxy-4'-n-butoxycarbonylphenyl)thiourea, N-p-cyanobenzoyl-N'-(3'-hydroxy-4'-n-amoxycarbonylphenyl)thiourea, and N-5-nitrofuroyl-N'(3'-hydroxy-4"-n-amoxycarbonylphrnyl)thiourea showed the growth inhibition of M. tuberculosis H/sub 37/Rv at the coccentraction og 10.mu.g/ml, respectively.

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Properties and Hair Growth Effect of Eugenol-Aspirin Derivative (유제놀의 아스피린 유도체에 관한 물성 및 육모효과)

  • Shin, Joon-Su;Kim, Jong-Ho;Kim, Kyoung-Soon;Youm, Jeong-Rok;Kim, Bak-Kwang
    • YAKHAK HOEJI
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    • v.41 no.5
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    • pp.571-574
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    • 1997
  • We have synthesized acetylsalicylic acid derivative of eugenol. And also, physico-chemical properties and analysis on this compound were examined. The correlation coefficient of the calibration curve in methanol solution was 0.9998. The hair growth stimulation of eugenol derivative on the hair of black mouse (C57BL/6), was also carried out using Implant method. When its ethanol solution was administered to the black mouse by route of skin, eugenol derivative promoted the growth of hair.

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Binding Properties of Guanosine-2',3',5' triisobutyrate

  • Yu, Byung-Sul;Kim, Kyoung-Mi;Sohn, Dong-Hwan
    • Archives of Pharmacal Research
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    • v.11 no.2
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    • pp.155-158
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    • 1988
  • To study the behavior of nucleic acid base in a nonpolar organic solvent, chloreform, we synthesized a derivative of guanosine. This erivative, guanosine-2', 3', 5'- trisobutyrate was obtained by reaction of guanosine with isobutyric anhydride, and identified by TLC, EA, IR and NMR. Hydrogen bonding specificity of this compound was revealed by IR and NMR. The molecules of guanosine 2',3',5'-trisobutyrate are self-associated in nonpolar solvent, and hydrogen bonds by imino protent become important as the concentration increases. In the presence of a cytosine derivative, the self-association of theguanosine drivative is destroyed, resulting from interaction with cytosine derivative.

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Synthesis and Biological Evaluation of Water-Soluble Oleanolic Acid Derivatives for use as Melanogenesis Inhibitors (멜라닌 생합성 억제제로서 수용성 Oleanolic Acid 유도체의 합성 및 활성 평가)

  • An, Hyun-Jin;Yoon, Young-kyung;Lee, Jae-Duck;Jeong, Noh-Hee
    • Applied Chemistry for Engineering
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    • v.31 no.6
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    • pp.653-659
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    • 2020
  • This study was focused on the synthesis of methoxy polyethylene glycol-oleanolic acid ester (mPEG-OA derivative) and investigation of its water solubility and anti-melanogenic effects. mPEG-OA derivative was identified by 1H and 13C NMR and FT-IR spectroscopic measurements. The water solubilities of mPEG-OA derivative and OA were found to be 13 and 0.013 mg/mL and that of mPEG-OA was found to be 1000-fold higher than that of OA. The effects of mPEG-OA derivative and OA on cell viability were measured using B16F10 melanoma cells. The viability of cells treated with mPEG-OA derivative (250 μM) increased 4-fold compared to that of cells treated with OA (62.5 μM). At mPEG-OA derivative and OA concentrations where the cell viability was unaffected, the inhibitory effect of mPEG-OA derivative and OA on the melanogenesis in B16F10 melanoma cells were 36 and 35% at 50 and 10 μM, respectively. The expression level of microphthalmia-associated transcription (MITF) was also reduced in B16F10 melanoma cells treated with mPEG-OA and OA. Overall, mPEG-OA derivative showed excellent water solubility and inhibitory effects of the melanogenesis, which could be used as a potential formulation for use in whitening functional cosmetic material.