• Bulletin of the Korean Chemical Society
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• v.22 no.6
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• pp.587-592
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• 2001

The potential anticancer agents new anthracycline derivatives (2~9) have been synthesized from daunomycin (1a) and doxorubicin (1b) ad starting materials. Compounds 2 and 6 were prepared by the nucleophilic displacement type esterification of a 14-bromodaunomycin (1c) with a acetylsalicylic and palmitic acid in triethylamine, respectively. Compound 3 and 7 were obtained from daunomycin (1a) by direct amidation with the corresponding acids in the presence of EDCI and PP as esterification regents. Whereas 4 and 8 were prepared by reaction of doxorubicin (1b) with one equivalent of acetylsalicylic and palmitic acid using DCC/DMAP, respectively, 5 and 9 were obtained from 1b by acylation with two equivalents of the corresponding acids using EDCI/PP reagents.

• 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.

• Archives of Pharmacal Research
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• v.17 no.3
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• pp.166-169
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• 1994

The anti-inflammatory activity of acetylsalicylic acid maltol ester (aspalatone), a potential anti-thombotic agent, was studied using the several experimental animal models of inflammation. By oral administration, aspalatone was found to possess the weak anti-inflammatory activity in models of an acute inflammation, in which aspalatone showed approximately one-third to one-fourth of the anti-inflammatory activity of aspirin. Aspalatone (200 mg/kg/day) and aspirin (50 mg/kg/day), however, did not show the inhibitory activity against granuloma fomation and adjuvant-induced arthritis.

• Journal of Korean Society of Environmental Engineers
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• v.39 no.7
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• pp.403-411
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• 2017

In this study, the occurrence and temporal variation of eight pharmaceuticals comprising antibiotics (clarithromycin, sulfathiazole, sulfamethazine, sulfamethoxazole, trimethoprim), scabicide (carbamazepine) and nonsteroidal anti-inflammatory drugs (acetylsalicylic acid, naproxen) in main stream and its tributary of the Nakdong River basin, were investigated. Concentrations of the target compounds ranged from $1.076{\mu}g/L$. The highest average concentration was observed for clarithromycin ($0.0316{\mu}g/L$), followed by sulfamethazine ($0.0170{\mu}g/L$), sulfamethoxazole ($0.0161{\mu}g/L$), naproxen ($0.0129{\mu}g/L$), carbamazepine ($0.0093{\mu}g/L$), acetylsalicylic acid ($0.0047{\mu}g/L$), sulfathiazole ($0.0024{\mu}g/L$) and trimethoprim ($0.0022{\mu}g/L$). The decreasing pattern of pharmaceutical concentrations was observed along with Nakdong River and the higher concentrations in downstream were observed than those in upstream. There was no temporal variation of the target compounds although the highest level was found in February. The calculated hazard quotients (HQs) for eight pharmaceuticals were below 1, indicating no environmental hazard in Nakdong River. However, further monitoring is still needed due to the other pharmaceuticals widely used in Korea.

• Journal of Pharmaceutical Investigation
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• v.39 no.1
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• pp.43-49
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• 2009

Aspirin or acetylsalicylic acid, a member of the salicylate family, is frequently used as an analgesic, antipyretic, anti-inflammatory and antiplatelet drug. Because aspirin is chemically unstable in water and heat for tablet formulation, additives including lubricants are used in preparing aspirin tablets, using a dry-granulation process. Aspirin tablets are produced by a number of manufacturers which usually use their own unique combination of additives during the manufacturing process. In this study, we employed an NMR based metabolomics technique to identify the manufacturers of various aspirin tablets. Aspirin tablets from six different companies were analyzed by 1H 400 MHz NMR. The acquired data was then integrated and processed by principal component analysis (PCA). Based on the NMR data, we were able to identify peaks corresponding to acetylsalicylic acid in all of the six samples, whereas different NMR patterns were found in the aromatic and aliphatic regions depending on the unique additive used. These observations led to the conclusion that the differences in the NMR patterns among the different aspirin tablets were due to the presence of additives.

• YAKHAK HOEJI
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• v.13 no.1
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• pp.1-15
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• 1969

A new method of qualitative and quantitative determination of barbiturates in the pharmaceuticals by means of $\alpha$-picoline-copper (II) was studied. Barbiturates in the pharmaceuticals were dissolved in the mixed solvent of 33% $\alpha$-picoline-Carbontetrachloride to yield Complex Compounds of barbiturates-copper (II)-$\alpha$-picoline. Complex Compounds of barbiturates show uniformly maximum absorption at the wavelength of 540m.mu. and wre to be identified at the concentration of 1 X 10$^{-4}$ Mole, and also was to be quantitatively determined at the concentration of 1 X 10$^{-3}$ Mole. By this method barbiturates in the pharmaceuticals could be determined in the presence of various compounds such as sulpyrine, isopropylantipyrine, antipyrine, phenacetin and etc. But Barbiturates could be also determined by this method after seperation with aminopyrine, acetaminophen, acetylsalicylic acid and etc. by column chromatography. And barbiturates and acetylsalicylic acid could be also determined by simultaneous equation while their complex compounds show uniformly each maximum absorption at the Wavelength of 540 m${\mu}$ and 620 m${\mu}$. I.R. spectra of these complex compounds show identification of Barbiturates derivatives. The composition ratio of these complex compounds were : barbiturates : Cu : ${\alpha}$-picoline=2:1:2.

• Natural Product Sciences
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• v.8 no.4
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• pp.147-151
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• 2002

In the course of our work on anti-platelet constituents from plants, eight phenolic compounds, $({\pm})-syringaresinol$ (1), 4-hydroxybenzaldehyde (2), 4-hydroxybenzoic acid (3), vanillic acid (4), 4-hydroxy cinnamic acid (5), quercetin 3-O-rhamnoside (6), rutin (7), and quercetin $3-(2^G-rhamnosylrutinoside)$ (8) were isolated from the methanol extract of the leaves of Magnolia obovata. The compounds were identified based on the spectroscopic data. Compound 2, 3, 5, 6, 7 and 8 were isolated for the first time from genus Magnolia. 1 and 6 showed same order of inhibitory potencies as acetylsalicylic acid (ASA) to rat platelet aggregation induced by all the stimulators tested. The remaining six compounds showed only mild effects.

• Archives of Pharmacal Research
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• v.27 no.4
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• pp.376-380
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• 2004

Five pentacyclic triterpenoids, oleanolic acid (1), hederagenin (2), ursolic acid (3), tormentic acid (4) and myrianthic acid (5), were isolated from the methanol extract of the leaves of Campsis grandiflora, and structures of the compounds were established by the spectroscopic methods. Compounds 2, 3, 4, and 5 were isolated for the first time from the genus Campsis. All of the compounds ($IC_{50}$: 45.3, 32.8, 82.6, 42.9 and $46.2{\mu}M$ respectively) were as equivalently inhibitive as acetylsalicylic acid ($IC_{50}:57.0{\mu}M$) on epinephrine induced platelet aggregation.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.206.1-206.1
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• 2003

From methanol extract of Acanthopnanax senticosus, six platelet anti-aggregating compounds, chiisanogenin (1), chiisanoside (2), ursolic acid (3), oleanolic acid (4), b-sitosterol (5) and daucosterol (6) were isolated. All of the isolated compounds showed dose-dependent inhibitory activities to rat platelet aggregation induced by all the agonist employed. Compound 1 showed about 50 folds higher potency than acetylsalicylic acid (ASA) on U46619 induced platelet aggregation (IC$\sub$50/ : 6.21 ${\mu}$M) and 10 ∼ 20 folds higher effect than ASA on epinephrine and arachidonic acid (AA) induced aggregation (IC$\sub$50/ ; 2.50 and 4.81 ${\mu}$M, respectively). (omitted)

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.235-235
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• 1994

NSAID의 대표적인 유도체인 acetylsalicylic acid(aspirin)은 항혈전 작용이 있다고 밝혀졌고, 주기적인 aspirin의 투여는 심근경색을 예방할 수 있음이 보고되었다. 그러나, 위궤양등 부작용의 발현이 심각하여 위의 목적에 입각한 aspirin의 장기적인 사용에 제약이 되고 있다. 이에 더욱 안전한 유도체인 aspalatone을 합성하였고, 이 물질은 낮은 궤양 유발능을 보이는 유망한 유도체로 개발중에 있다. 본 연구는 aspalatone의 in vivo 항염증 활성을 밝히기 위하여 시행하였다.