• Archives of Pharmacal Research
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• 제14권1호
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• pp.48-51
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• 1991

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.

• Archives of Pharmacal Research
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• 제15권2호
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• pp.184-186
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• 1992

Malonic acid amides were synthesized using different amino acids and their esters. THe synthesized compounds were evaluated for their sedative activity on rats. Potentiating effect of all the compounds on pentobarbitone induced sleep on rats was observed. Plasma protein binding studies were also carried out and it was observed that the synthesized compounds have low plasma protein binding as compared to barbiturates.

• Journal of Pharmaceutical Investigation
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• 제14권4호
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• pp.145-155
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• 1984

The use of stable isotope compounds in pharmaceutical research was described with recent 33 references, which include synthesis, selected ion monitoring, pharmacokinetics, drug metabolism, and mechanism of drug action.

• 대한화학회지
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• 제55권6호
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• pp.960-968
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• 2011

A series of isonicotinyl hydrazones and their 4-thiazolidinones have been synthesized by condensation of isonicotinic acid hydrazide with various aromatic aldehydes to yield Schiff's bases, followed by the cyclocondensation of Schiff's bases with 2-mercaptoacetic acid to yield their 4-thiazolidinones. The synthesized compounds have been characterized by their elemental, analytical and spectral studies. All these compounds were evaluated for their invitro antimicrobial activity against a spectrum of non-resistant and resistant microbial organisms. These studies proved that compounds 5e,i against B. subtilis; 5e,f,h against B. anthracis; 5g,i against S. aureus showed good activity at lower concentrations. Compounds 5d-5i displayed significant activity against resistant strain of K. pneumonia with minimum inhibitory potency in the concentration range of 2-16 ug/ml.

• Natural Product Sciences
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• 제26권2호
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• pp.158-164
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• 2020

Helicobacter pylori is a well-known pathogen that is responsible for gastric disorders. Overcoming of the antibiotic-resistance is a main barrier to treat H. pylori infection. In our search for anti-H. pylori compounds from natural resources, bioactivity-guided isolation on the ethyl acetate fraction of Fraxinus mandshurica bark that had shown anti-H. pylori activity gave twelve compounds (1 - 12) of six coumarins, three phenylethanoids, two secoiridoids, and a lignan using silica gel column chromatography, Sephadex-LH 20, and recrystallization. The chemical structures were identified by spectroscopic data analysis, including 1D, 2D NMR, and mass spectrometry. Among them, compounds 2, 10, and 11 showed moderate growth inhibitory activity against three strains of H. pylori, compared with positive controls of quercetin and metronidazole. Compounds 5, 6, 8, and 12 exhibited the inhibitory activity against strains 26695 or 43504. This is the first report on the anti-H. pylori activity of this plant and the isolated compounds.

• Bulletin of the Korean Chemical Society
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• 제31권8호
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• pp.2345-2350
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• 2010

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives of these moieties were evaluated for antimicrobial activity. Most of the synthesized compounds showed good antimicrobial activity at 200 and $100\;{\mu}g/mL$. Compounds showed most significant antibacterial activity against gram negative test organism Escherichia coli and most significant antifungal activity against test organisms Aspergillus niger and Candida albicans. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] were more potent against microbes as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.1011-1016
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• 2011

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• 대한환경공학회지
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• 제33권6호
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• pp.453-479
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• 2011

오늘날 전세계적으로 수환경에서의 잔류 의약물질들의 오염에 대한 연구결과들이 많이 보고되고 있다. 이들 잔류 의약물질들은 다양한 종류와 그들이 가지는 물리 화학적인 특성들로 인해 수환경에서의 거동, 오염현황, 영향 및 독성 등도 매우 다양하여 수환경 및 수처리 공정에서의 거동을 예측 평가하기가 어렵다. 선진 외국의 경우 환경 중에서의 오염 현황 및 사용량을 정량화하기 위한 조사를 이미 시작하였고, 잔류 의약물질들의 인체에 대한 잠재적 위험성뿐만 아니라 상수나 하수처리 공정에서의 제거기술에 관한 다양한 연구도 활발히 진행하고 있다. 그러나 국내의 경우 잔류 의약물질들에 대해 전국 주요하천과 상수원에 대한 모니터링 결과도 매우 부족한 실정이다. 우선 국내의 경우는 상수원으로 이용되는 전국 주요 하천과 호소에 대해 주기적이고 체계적인 오염현황 평가가 선행되어야 하며, 잔류 의약물질들이 비교적 고농도로 검출되는 상수원에 대해서는 주오염원에 대한 조사도 병행되어야 한다. 또한, 의약물질 사용량은 지속적으로 증가할 것으로 전망되기 때문에 하수처리 시설에 대한 부하도 지속적으로 증가할 것이다. 따라서 수환경에서의 유해도를 저감시키기 위해 효과적인 하수처리 공법의 도입이 절실하며, 상수에 대한 안전성 확보를 위해서도 잔류 의약물질들의 수환경중에서의 물리 화학적 거동에 대한 면밀한 연구가 요구된다.

• 대한약침학회지
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• 제25권3호
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• pp.199-208
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• 2022

Objectives: In recent decades, the trend for treating diabetes mellitus (DM) has shifted toward alternative medicines that are obtained from plant sources. Existing literature suggests that phenolic compounds derived from plants possess promising health-promoting properties. This study aimed to discuss the role of plant-derived phenolic compounds in the effective treatment and management of diabetes. Methods: Information about plant secondary metabolites, phenolic compounds, and their role in the treatment and management of diabetes was collected from different databases, such as Pubmed, ScienceDirect, Scopus, and Google Scholar. Keywords like secondary metabolites, phenolic compounds, simple phenol, flavonoids, lignans, stilbenes, and diabetes were searched. Research and review articles with relevant information were included in the study. Results: Anti-diabetic studies of the four major classes of phenolic compounds were included in this review. The plant-derived phenolic compounds were reported to have potent anti-diabetic activities. However, each class of phenolic compounds was found to behave differently according to various mechanisms. Conclusion: The obtained results suggest that phenolic compounds derived from natural sources display promising anti-diabetic activities. Based on the available information, it can be concluded that phenolic compounds obtained from various natural sources play key roles in the treatment and management of diabetes.

• Archives of Pharmacal Research
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• 제27권2호
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• pp.169-172
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• 2004

Activity-guided fractionation of the EtOAc-soluble extract of the stems of Couepia ulei, using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells led to the isolation of two active compounds, a new natural product, erythro-2,3-bis(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-o1 (1), and a known compound, evofolin-B (2), along with five inactive compounds all of known structure, viz., betulinic acid, oleanolic acid, pomolic acid, ($\pm$)-syringaresinol, and ursolic acid. These isolates were identified by analysis of physical and spectral data. Compounds 1 and 2 exhibited QR inducing activity, with observed CD (concentration required to double induction) values of 16.7 and 16.4 $\mu\textrm{M}$, respectively.