• Title/Summary/Keyword: Pharmaceutical analysis

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Thiadiazole Derivatives as Potential Anticonvulsant Agents

  • Mullick, Pooja;Khan, Suroor A.;Verma, Surajpal;Alam, Ozair
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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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)].

Synthesis of Some New Biologically Active Benzothiazole Derivatives Containing Benzimidazole and Imidazoline Moieties

  • Chaudhary, Manish;Pareek, Deepak;Pareek, Pawan K.;Kant, Ravi;Ojha, Krishan G.;Pareek, Arun
    • Bulletin of the Korean Chemical Society
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    • v.32 no.1
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    • pp.131-136
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    • 2011
  • Synthesis of N-(1H-benzimidazol-2-yl)-6-substituted-1,3-benzothiazol-2-amines and 6-substituted-N-(4,5-dihydro-1H-imidazol-2-yl)-1,3-benzothiazol-2-amines by the reaction of substituted 2-aminobenzothiazoles with carbon disulphide and methyl iodide followed by the reaction with o-phenylene diamine/ethylene diamine are reported. All the synthesized compounds were characterized by elemental analysis, IR spectra and $^1H$ NMR spectral studies. The potent antibacterial and entomological (antifeedant, acaricidal, contact toxicity and stomach toxicity) activities of the synthesized compounds were investigated.

Studies on the Condensation with Malonates and Urea (Malon 산 Ester 유도체와 요소와의 축합에 관한 연구)

  • 국채호;조윤상;주상섭
    • YAKHAK HOEJI
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    • v.18 no.2
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    • pp.125-132
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    • 1974
  • The by-products which were occured in the synthesis of 5-ethyl-5-phenyl barbituric acid were isolated by column chromatography combined with gas-liquid chromatography and were identified by elemental analysis, ir, nmr and mass spectroscopy ; major by-products were ethyl${\alpha}$-phenylbutyrate and ${\alpha}$-phenylbutyramide. The alkoxide which was known to be a condensation agent not only accelerated the condensation but also did the decarboxylation. And the entity concenrned with the condensation with diethyl ethylphenylmalonate was not urea but N-monosodium urea.

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Identification of a Cryptic Type III Polyketide Synthase (1,3,6,8-Tetrahydroxynaphthalene Synthase) from Streptomyces peucetius ATCC 27952

  • Ghimire, Gopal Prasad;Oh, Tae-Jin;Liou, Kwangkyoung;Sohng, Jae Kyung
    • Molecules and Cells
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    • v.26 no.4
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    • pp.362-367
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    • 2008
  • We identified a 1,134-bp putative type III polyketide synthase from the sequence analysis of Streptomyces peucetius ATCC 27952, named Sp-RppA, which is characterized as 1,3,6,8-tetrahydroxynaphthalene synthase and shares 33% identity with SCO1206 from S. coelicolor A3(2) and 32% identity with RppA from S. griseus. The 1,3,6,8-tetrahydroxynaphthalene synthase is known to catalyze the sequential decarboxylative condensation, intramolecular cyclization, and aromatization of an oligoketide derived from five units of malonyl-CoA to give 1,3,6,8-tetrahydroxynaphthalene, which spontaneously oxidizes to form 2,5,7-trihydroxy-1,4-naphthoquinone (flaviolin). In this study, we report the in vivo expression and in vitro synthesis of flaviolin from purified gene product (Sp-RppA).

Climate Change Disclosure Performance of Pharmaceutical Industry of Bangladesh

  • DAS, Shaily;JENI, Fatema Akter
    • Asian Journal of Business Environment
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    • v.11 no.4
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    • pp.39-45
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    • 2021
  • Purpose: This study is designed to investigate the extent and nature of climate change disclosure of listed pharmaceutical companies of Bangladesh. Research design, data and methodology: In order to perform this research, a content analysis methodology is used. A climate change disclosure index is constructed to examine 12 different climate change disclosure issues. Information is collected from the annual reports of 29 pharmaceutical companies listed on the Dhaka Stock Exchange for the year 2019. Results: This study finds that only 48.28% of the sample companies provided disclosure on at least one issue regarding climate change. 'Energy savings' is the mostly disclosed issue whereas 'Pollution control expenditure', 'Biodiversity conservation initiatives' are the least disclosed issues. Research implication: This study concludes 64.29% of the companies examined, use less than five sentences for climate change disclosure, which depicts unsatisfactory disclosure practices regarding climate change issues. Study findings would be helpful for different industries of Bangladesh to implement efficient climate change reporting Practice. Future studies can be conducted on other industries to obtain more comprehensive result.

Structure Elucidation and Antibacterial Activity of Oxazolomycin Family KSM-2690 B Derived from Actinomycete Collected in Jeju Island (제주도 방선균 유래 oxazolomycin 계열 KSM-2690 B의 구조 결정과 항균활성에 관한 연구)

  • Hyeongju Jeong;Jooyoung Kim;Soohyun Um;Kyuho Moon
    • Korean Journal of Pharmacognosy
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    • v.54 no.1
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    • pp.16-20
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    • 2023
  • KSM-2690 B (1), a peptide-polyketide hybrid compound, was discovered from an actinomycete strain (CJD 1) isolated from Dong-Baek hill on Jeju Island, Republic of Korea. The chemical structure of 1 was identified by using NMR, MS, and UV spectroscopic analyses. Careful analysis of 1D and 2D NMR data revealed that KSM-2690 (1) has an oxazole ring, a β-lactone-γ-lactam spirocycle ring, and both triene and diene structures. KSM-2690 B (1) showed inhibitory activities against E. coli at 200 ㎍/mL.

Analysis of Gender Differences in Physician's Desk Reference (Physician's Desk Reference에 나타난 성별차이 분석)

  • Heo, Jung-Sun;Kim, Kyung-Hee;Yoon, In-Kyung;Kim, Hyun-Ju;Kim, You-Jin;Choi, Jong-Min;Lee, Byeong-Gu;Lee, Hwa-Jeong;Gwak, Hye-Sun
    • Korean Journal of Clinical Pharmacy
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    • v.21 no.1
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    • pp.22-29
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    • 2011
  • Purpose: This study aims to investigate how gender-based differences are actually reflected on drug approval. Methods: Data on gender-based differences of drugs were analyzed by searching PDR (Physician's Desk Reference) with the keyword, "GENDER". Results: There were descriptions related to gender in product directions of 361 drugs in 2009 PDR, out of which 63 items actually showed gender-related differences. Drug categories showing comparatively high gender-based differences were nervous system, cardiovascular system, and alimentary tract and metabolism. Pharmacokinetic differences between genders were observed most frequently; compared to men, 32 drugs showed higher absorption while 18 drugs revealed lower clearance in women. There were 2 drugs which gender should be considered before prescribing, and 5 drugs which showed different severity of adverse effects according to gender. Conclusions: It is necessary to establish domestic policies for drug approval and use which reflects gender-based differences through sufficient researches.

In vivo and In vitro Metabolism of Recombinant Human Epidermal Growth Factor (DWP401) in Rats (재조합 인간 상피세포성장인자(DWP401)의 흰쥐에서의 in vivo와 in vitro 대사)

  • Koh, Yeo-Wook;Nam, Kouen-Ho;Jung, Ju-Young;Park, Seung-Kook;Yu, Young-Hyo;Kim, Jae-Hwan;Han, Kun;Park, Myung-Hwan;Shim, Chang-Koo
    • YAKHAK HOEJI
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    • v.41 no.3
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    • pp.381-388
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    • 1997
  • Metabolism of DWP401, recombinant juman epidermal growth factor, was examined in vivo and in vitro in rats. When $^{125}I$-labeled DWP401 was administered at a dose of 50 ${\mu}g$/kg by i.v. injection. $^{125}I$-labeled DWP401 was rapidly degraded within 30 minytes above 93%. Thin layer chromatography analysis of urine collected for 24 hr after i.v. administration of $^{125}I$-labeled DWP401 showed ohly one spot on a X-ray film which was considered as diiodo-tyrosine. This result suggests tha $^{125}I$-labeled DWP401 was completely digested into free amino acids without any specific intermediate polypeptides. About 42.1% of the administered iodine was recovered in 24 hr. For in vitro degradation study, $^{125}I$-labeled DWP401 was added to plama and tissue homogenates of rats and incubated at $37^{\circ}C$. Almost 98% of the added radioactivity recovered from the protein fraction of the liver, kidey, small intestine, stomach and spleen decreased rapidly. For examplem the recovery rates of $^{125}I$-labeled DWP401 were 58.6, 63.2, 39.9, 52.9 and 66.8% after 4hrs of incubation in respective organ homogenates.

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FADD Phosphorylation Modulates Blood Glucose Levels by Decreasing the Expression of InsulinDegrading Enzyme

  • Lin, Yan;Liu, Jia;Chen, Jia;Yao, Chun;Yang, Yunwen;Wang, Jie;Zhuang, Hongqin;Hua, Zi-Chun
    • Molecules and Cells
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    • v.43 no.4
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    • pp.373-383
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    • 2020
  • Our previous study revealed a novel role of Fas-associated death domain-containing protein (FADD) in islet development and insulin secretion. Insulin-degrading enzyme (IDE) is a zinc metalloprotease that selectively degrades biologically important substrates associated with type 2 diabetes (T2DM). The current study was designed to investigate the effect of FADD phosphorylation on IDE. We found that the mRNA and protein levels of IDE were significantly downregulated in FADD-D mouse livers compared with control mice. Quantitative real-time polymerase chain reaction analysis showed that FADD regulates the expression of IDE at the transcriptional level without affecting the stability of the mRNA in HepG2 cells. Following treatment with cycloheximide, the IDE protein degradation rate was found to be increased in both FADD-D primary hepatocytes and FADD-knockdown HepG2 cells. Additionally, IDE expression levels were reduced in insulin-stimulated primary hepatocytes from FADD-D mice compared to those from control mice. Moreover, FADD phosphorylation promotes nuclear translocation of FoxO1, thus inhibiting the transcriptional activity of the IDE promoter. Together, these findings imply a novel role of FADD in the reduction of protein stability and expression levels of IDE.