• Title/Summary/Keyword: Biological synthesis

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The Reaction of Digitoxin and Digoxin with Cyanoacetic Acid Hydrazide: Synthesis of Coumarin, Thiazole, Thiophene and Pyridine Derivatives with Potential Biological Activities

  • Doss, Senot H.;Wardakhan, Wagnat W.;Louca, Nadia A.
    • Archives of Pharmacal Research
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    • v.24 no.5
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    • pp.377-384
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    • 2001
  • The reaction of either Digitoxin or Digoxin with cyanoacetic acid hydrazide gave the hydrazone derivatives 3a and 3b respectively. The reactivity of the latter products towards chemical reagents was studied to give heterocyclic derivatives with potential biological activities.

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Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects (Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색)

  • 신혜순;이희주
    • Biomolecules & Therapeutics
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    • v.3 no.3
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    • pp.217-222
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    • 1995
  • Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

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Synthesis of Oxazolidinone Phosphonate Derivatives, Part I

  • Hwang, Jae-Min;Shin, Woon-Seob;Jung, Kang-Yeoun
    • Bulletin of the Korean Chemical Society
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    • v.25 no.9
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    • pp.1326-1330
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    • 2004
  • Several new derivatives of oxazolidinone phosphonate, that are expected to show biological activity, were prepared efficiently by previously published methods. ${\gamma}$-Ketophosphonate 1 was synthesized using pentacovalent oxaphosphorane chemistry followed by reductive amination with aromatic amine of oxazolidinone 4. Biological activity of the synthetic compounds has been studied. One of the synthetic compounds showed promising result for us to pursue further studies.

Total Synthesis of (R,Z)-(-)-5-Tetradecen-4-olide, the Pheromone of the Japanese Beetle and Its Biological Activity Test

  • Kang, Suk-Ku;Shin, Dong-Soo;Lee, Jeong-Oon;Goh, Hyun-Gwan
    • Bulletin of the Korean Chemical Society
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    • v.7 no.6
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    • pp.444-447
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    • 1986
  • Optically active (R,Z)-(-)-5-tetradecen-4-olide, the pheromone of Popillia japonica Newman was synthesized from (R)-2,3-O-isopropylideneglyceraldehyde as starting material. The biological activity test of the synthetic pheromone as attractant for the male Japanese beetle was tested in Korea.

The synthesis of aminocarbocyclics from glucose

  • Shin, Dong-Hyouk;Jeong, Jin-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.235.1-235.1
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    • 2003
  • The abundance of carbohydrates in nature with diverse roles in biological systems makes them a subject of considerable interest. They exhibit biological effects. ranging from cellular regulation to the selective inhibition of enzymes with key roles in living organisms. A wide range of carbocyclic polyhydroxyls has significant therapeutic effects, examples of which include cyclohexane hexitols, such as inositols, and pseudo-sugars, such as cyclophellitol and valienamine. (omitted)

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Synthesis and Biological Effects of 2, 3-Diphenyl-5-Methoxyindole and Substituted Benzophenone Derivatives

  • Hishmat, O.H.;El-Sbabrawy, O.A.;Nakkady, S.S.;Mahmoud, S.S.
    • Archives of Pharmacal Research
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    • v.12 no.3
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    • pp.149-153
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    • 1989
  • Seven 2, 3-diphenyl-5-methoxyindole derivatives were synthesized. The effect of structural variation of these molecules on biological activities was examined. None of the tested compounds was found to be toxic up 5 gm/Kg body weight. Four compounds demonstrated smooth muscle relaxant effects and one showed a persistent hypotensive effect. Only the parent compound, 2, 3-diphenyl-5-methoxyindole, showed a significant analgesic effect.

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Role of $Ca^{2+}$ and Calmodulin on the Initiation of Sperm Motility in Salmonid Fishes

  • Kho, Kang-Hee;Morisawa, Masaaki;Choi, Kap-Seong
    • Journal of Microbiology and Biotechnology
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    • v.14 no.3
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    • pp.456-465
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    • 2004
  • $K^+$ efflux through a certain type of $K^+$ channels causes the change of membrane potential and leads to cAMP synthesis in the transmembrane cell signaling for the initiation of sperm motility in the salmonid fishes. The addition of $Ca^{2+}$ conferred motility to the trout sperm that were immobilized by external $K^+$ and other alkaline metals, $Rb^+$ and $Cs^{2+}$, suggesting the participation of external $Ca^{2+}$ in the initiation of sperm motility. L-type $Ca^{2+}$ channel blockers such as nifedipine, nimodipine, and FS-2 inhibited the motility, but N-type $Ca^{2+}$ channel blocker, w-conotoxin MvIIA, did not. On the other hand, the membrane hyperpolarization and cAMP synthesis were suppressed by $Ca^{2+}$ channel blockers, nifedipine, and trifluoroperazine. Furthermore, these suppressions were relieved by the addition of $K^+$ ionophore, valinomycin. Inhibitors of calmodulin, such as W-7, trifluoperazine, and calrnidazol-C1, inhibited the sperm motility, membrane hyperpolarization, and cAMP synthesis. The results suggest that $Ca^{2+}$ influx through $Ca^{2+}$ channels that are sensitive to specific $Ca^{2+}$ channel blockers and calmodulin participate in the changes of membrane potential, leading to synthesis of cAMP in the cell signaling for the initiation of trout sperm motility.

Effectiveness of Krill Oil in Regulating Skin Moisture

  • Yoon-Seok Chun;Jongkyu Kim;Ji-Hoon Lim;Namju Lee;Sae-kwang Ku
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.359-368
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    • 2023
  • This study aims to explore the impact of Krill Oil (KO, SuperbaTM Boost) on skin moisturization regulation. The research involved five groups: an intact control, a reference group (L-AA 100 mg/kg), and KO groups (400, 200, and 100 mg/kg), each comprising ten mice. Oral administration was conducted for 8 weeks (56 days), during which changes in body weight, hyaluronan, collagen type 1 (COL1), transforming growth factor-β1 (TGF-β1), ceramide, and water contents were analyzed in dorsal back skin tissue. Real-time PCR was employed to assess gene expression related to hyaluronic acid synthesis (HAS1, HAS2, HAS3), COL1 synthesis (COL1A1 and COL1A2), and TGF-β1. Results demonstrated that KO administration significantly increased hyaluronan content, hyaluronic acid synthesis (HAS1, HAS2, HAS3), COL1 content, COL1 synthesis (COL1A1 and COL1A2), TGF-β1 content, TGF-β1 mRNA expression, ceramide content, and water content in a concentration-dependent manner compared to the intact control. Importantly, no discernible disparities were noted between the KO and L-AA groups, even though they received equivalent oral dosages. This study accentuates the potential utility of exogenous KO in the regulation of skin moisture, thus positioning it as a promising avenue for the development of nutricosmetics. Future research endeavors should delve into the role of KO in safeguarding against both intrinsic and extrinsic aging-related skin manifestations, as well as its potential to ameliorate skin wrinkles, in conjunction with its moisturizing attributes.

Improved Cell Viability of Lactobacillus crispatus KLB46 by Stress Adaptation (Lactobacillus crispatus KLB46의 스트레스 전처리시 열 내성 증진효과)

  • Kwak, Dae-Yung;Kang, Chang-Ho;Jeon, HanEul;So, Jae-Seong
    • KSBB Journal
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    • v.29 no.2
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    • pp.81-86
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    • 2014
  • Lactobacilli, the dominant species of microorganisms in the vaginal flora of healthy women, play important roles to prevent bacterial vaginosis and other sexually transmitted diseases. In this study, we carried out studies on stress adaptation prior to various stress treatment. We found that heat or salt adapted KLB46 showed higher cell viability than non adapted upon heat stress at $60^{\circ}C$ for 20 min. When chloramphenicol was added during the adaptation process, heat tolerance was abolished. This result suggested that de novo protein synthesis was essential during adaptation.

A study of aldol condensation reaction product using a microreactor (마이크로 반응기를 적용한 알돌 축합반응 생성물 제조연구)

  • Kim Young-Jun;Lee Sang-Seo;Son Sung-Kwang;Song Kwang-Ho;Choe Jae-Hoon
    • Proceedings of the Korean Society of Precision Engineering Conference
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    • 2006.05a
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    • pp.543-544
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    • 2006
  • 3-methyl-2-cyclopentenone is a valuable reaction intermediate for various high value added products. 3-methyl-2-cyclopentenone is not only expensive but also difficult to produce. 3-methyl-2-cyclopentenone can be synthesized by base catalyzed intermolecular aldol condensation. In this work, we studied a simple and practical method for synthesizing 3-methyl-2-cyclopentenone. Experimental results showed the advantages of the continuous flow process using a microreactor with kenic mixers for the synthesis of 3-methyl-2-cyclopentenone.

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