• Bulletin of the Korean Chemical Society
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• 제22권6호
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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.

• 약학회지
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• 제41권5호
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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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• 제17권3호
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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.

• 대한환경공학회지
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• 제39권7호
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• pp.403-411
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• 2017

본 연구는 낙동강 본류와 연계한 지천중심을 대상으로 항생제(clarithromycin, sulfathiazole, sulfamethazine, sulfamethoxazole, trimethoprim), 항정간제(carbamazepine), 진통제(acetylsalicylic acid, naproxe)를 포함한 8종의 의약물질의 현황 및 시기별 변화에 대해 조사를 실시하였다. 조사 대상물질의 검출 수준은 $1.076{\mu}g/L$까지 나타났으며, 조사 대상물질에서 clarithromycin($0.0316{\mu}g/L$)이 가장 높은 평균 농도로 검출되었고, 다음으로 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 ($0.0024{\mu}g/L$), trimethoprim ($0.0022{\mu}g/L$) 순으로 나타났다. 낙동강 수계의 지점별 검출 수준은 하류의 농도수준이 상류의 검출 농도보다 상대적으로 높게 나타났다. 2월 조사시기에서 높은 검출 수준을 보였으나, 시기별 차이는 뚜렷하게 나타나지 않았다. 대상 의약물질 8종의 유해지수를 산정한 결과 모두 1보다 낮은 값을 나타내어 낙동강 수계에 미치는 생태위해성은 낮은 것으로 평가되었으나 추후 본 연구대상 물질 외 사용되고 있는 다른 의약물질로 확장 한 연구가 더 수행될 필요가 있는 것으로 판단된다.

• Journal of Pharmaceutical Investigation
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• 제39권1호
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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.

• 약학회지
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• 제13권1호
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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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• 제8권4호
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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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• 제27권4호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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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)

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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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.