• Title/Summary/Keyword: Active ester

검색결과 160건 처리시간 0.025초

Ester형 Chloramphenicol의 생체내 대사에 대하여 (Metabolic fate of chloramphenicol-ester)

  • 한병훈
    • 약학회지
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    • 제8권1호
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    • pp.1-5
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    • 1964
  • Present experiment in vivo shows that some conversions of active groups in chloramphenicol residue of ester, that is hydrolytic cleavage of dichloracetamide and glucuronide formation, seem to take place prior to hydrolysis. This result suggest that the enzymatic hydrolysis rate in vitro, is not available as an index for the evaluation of the chlorampherical ester potency.

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광학 활성 2-Amino-3-Phosphonopropionic Acid의 새로운 합성 방법과 그를 포함하는 펩티드의 합성 (Synthesis of Peptides Containing Optically Active 2-Amino-3-Phosphonopropionic Acid)

  • 김상범;조성기;한정식;김용준;홍석인
    • 대한화학회지
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    • 제38권7호
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    • pp.516-520
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    • 1994
  • L-serine으로부터 광학 활성을 가지는 2-amino-3-phosphonopropionic acid를 새로운 방법으로 합성하였으며 2-amino-3-(diethylphosphono)-propionic acid methyl ester를 아미노산과 축합시켜 광학 활성을 갖는 새로운 포스포노트리펩티드를 합성하였다.

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Development of an Isolable Active Ester, Diethyl Thiophosphoryl [(Z)-(2-Aminothiazol-4-yl)-2-(Methoxyimino)acetate (DAMA) for the Synthesis of Cefotaxime

  • Yoon, Man-Young;Lee, Hee-Bong;Shin, Hyun-Ik
    • Bulletin of the Korean Chemical Society
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    • 제32권2호
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    • pp.407-410
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    • 2011
  • An isolable activated ester, diethyl thiophosphoryl [(Z)-(2-aminothiazol-4-yl)-2-(methoxyimino)acetate (9a, DAMA) was prepared in high purity, which was at least stable for 7 d at $25^{\circ}C$ and 6 months at $5^{\circ}C$. Its reaction with 7-ACA (4) in the presence of tributylamine in i-PrOH provided cefotaxime (1) of high purity in good yield. Preparation of DAMA and its reaction with 7-ACA (4) to 1 was performed in one-pot manner, respectively with minimal unit operations of stirring and filtration.

Antioxident components from Aralia continentalis

  • Kim, Ju-Sun;Kang, Sam-Sik;Park, Jae-Sue
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.182-182
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    • 1998
  • The root of Aralia continentalis Kitagawa(Araliaceae) have been used as an analgesic and fever remedy, and for treatment of rheumatism in Chinese medicine, whereas the young leaves are used for salad. An antioxidant activity of the young leaves of A continentalis was determined by measuring lipid peroxide produced when a mouse liver homogenate was exposed to the air at 37$^{\circ}C$, using 2-thiobarbituric acid(TBA) and by evaluation the radical scavenging activity on 1,l-diphenyl-2 picrylhydrazyl (DPPH) radical. Bioassay guided fractionation of MeOH extract isolated six flavonoid compounds as active components from EtOAc fraction. Adenosine and two saponins were isolated from the weak active BuOH fraction. The antioxidant effect by DPPH radical scavenging activity showed that quercetin was the most active among these compounds. Hyperoside and kaempferol were also active, while 6"-O-acetyl astragalin, astragalin, trifolin, adenosine, oleanolic acid 28-O-glucosyl ester and salsoloside C methyl ester were almost inactive. All the compounds were identified by spectroscopic methods.

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(2S,3R)-3-하이드록시호모세린락톤의 입체선택적 합성 : 바이닐글라이신 OBO Ester 유도체의 입체선택적인 이중알콜화 반응 (Stereoselective Synthesis of (2S,3R)-3-Hydroxyhomoserine Lactone via anti Selective Dihydroxylation of an OBO Group-Protected Vinyl Glycine Analog)

  • 고무현;전종호;김영규
    • 공업화학
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    • 제31권2호
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    • pp.187-192
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    • 2020
  • (2S,3R)-3-hydroxyhomoserine lactone (HSL)은 생리학적 활성을 가지는 다양한 종류의 화합물을 합성하기 위한 중간체로 활용되어 왔다. 본 논문에서는 OBO ester로 보호된 바이닐글라이신 유도체에 이중알콜화 반응을 수행하여 효율적인 HSL 합성 결과를 보고하고자 한다. 바이닐글라이신의 비고리 conformation은 크기가 큰 OBO ester에 의해 조절되었으며 N-inside conformation을 통해 이중알콜화 반응이 진행됨으로써 높은 anti 선택성(> 10 : 1)을 얻을 수 있었다. 이러한 결과를 바탕으로 N-Cbz-L-serine을 출발물질로 사용하여 총 7단계 34%의 수율로 HSL을 합성할 수 있었다. 본 연구의 결과는 amino diol 구조를 가지는 다양한 생리활성 천연물들의 입체선택적인 합성에 유용하게 활용될 수 있을 것으로 기대된다.

고분자(高分子) 계면활성제(界面活性劑)에 관(關)한 연구(硏究) (제(第) 2 보(報));나트륨 알파 술폰 지방산(脂肪酸) 비닐에스테르 올리고머류(類)의 계면활성(界面活性) (Studies on the Polymeric Surface Active Agent (II);Synthesis Activities of Sodium ${\alpha}-Sulfo$ Fatty Acid Vinyl Ester Oligomers)

  • 정노희;남기대;소부영;소희준
    • 한국응용과학기술학회지
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    • 제6권1호
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    • pp.51-57
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    • 1989
  • A series of four sodium ${\alpha}-sulfo$ fatty vinyl ester oligomers including sodium ${\alpha}-sulfo$ lauric acid vinyl ester oligomer, sodium ${\alpha}-sulfo$ myristic acid vinyl ester oligomer, sodium ${\alpha}-sulfo$ palmitic acid vinyl ester oligomer and sodium ${\alpha}-sulfo$ stearic acid vinyl ester oligomer were examined for surface activities such as surface tension, foaming power, foam stability, emulsifying power, dispersion effect, solubilization of orange OT. The critical micelle concentration(CMC) was also evaluated. Consequently, these sodium ${\alpha}-sulfo$ fatty acid vinyl ester oligomers were shown to have a good cohesive power and dispersion effect.

고분자(高分子) 계면활성제(界面活性劑)에 관(關)한 연구(硏究)(제(第) 1 보(報));나트륨 알파 술폰 지방산(脂肪酸) 비닐에스테르 올리머고류(類)의 합성(合成) (Studies on the Polymeric Surface Active Agent (I);Synthesis of Sodium ${\alpha}-Sulfo$ Fatty Acid Vinyl Ester Oligomers)

  • 정노희;노승호;남기대;소부영
    • 한국응용과학기술학회지
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    • 제6권1호
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    • pp.21-26
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    • 1989
  • Four fatty acid vinyl esters were synthesized by transesterification between vinyl acetate and lauric acid, myristic acid, palmitic acid, stearic acid, respectively. Fatty acid vinyl ester oligomers were prepared from polymerization of four fatty acid vinyl esters in the presence of potassium persulfate in methanol. The ${\alpha}-sulfonation$ of these four fatty acid vinyl ester oligomer were carried by direct addition of sulfur trioxide. Especially, molecular weights of sodium ${\alpha}-sulfo$ fatty acid vinyl ester oligomers were measured by boiling point method.

Cefazolin Butyrolactone Ester의 합성 및 생물약제학적 연구 (Synthesis and Biopharmaceutical Studies of Cefazolin Butyrolactone Ester, a Novel Prodrug of Cefazolin)

  • 이진환;조행남;최준식
    • 약학회지
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    • 제47권5호
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    • pp.331-338
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    • 2003
  • A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.