• 제목/요약/키워드: synthetic activity

검색결과 971건 처리시간 0.028초

Synthetic $\beta$-Lactam Antibiotics V. Antibacterial Activity of Some 7$\beta$[2-(2-Aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(quinolinium)thiomethylcephalosporins

  • Lim, Dong-Yeol;Park, Sang-Woo;Kim, You-Seung
    • Archives of Pharmacal Research
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    • 제14권3호
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    • pp.279-281
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    • 1991
  • In the field of cephalosporins, introduction of quaternary heterocyclic methyl goups at the C-3 position has led to a new class of cephalosporins such as cefepime and cefpirome, the so-called 4th generation cephalosporins which are characterized by their potent activity. Since than many efforts were attempted to synthesize more effective analogs.

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Chloramphenicol과 해열제와의 Ester화합물에 관한 약제학적 연구 (I) (Pharmaceutical Studies on the Esterification of Chloramphenicol with Antipyretics (I))

  • 김정우;김종갑
    • 약학회지
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    • 제27권3호
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    • pp.207-213
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    • 1983
  • Chloramphenicol (CAF) was esterified with aspirin, naproxen and acetaminophen in order to develop new prodrugs which have double effect-antibiotic activity and antipyretic effect. Chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate (CAF-NAX), and chloramphenicol acetaminophen succinate (CAF-SUC-ACET) were synthesized by using dicyclohoxylcarbodiimidc (D.C.C.) because of two hydroxyl group of chloramphenicol. Three synthetic prodrugs did not show bitterness and antibiotic activity in vitro, and were hydrolyzed in liver homogenate, but weren't in acid.

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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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    • 제7권6호
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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.

호박벌 유래 디펜신 유전자의 분자적 특성분석 및 항균 활성 (Antimicrobial activity and characterization for defensin of synthetic oligopeptides derived from Bombus ignitus)

  • 강희윤;김인우;이준하;권용남;윤은영;윤형주;김성렬;김익수;황재삼
    • 한국잠사곤충학회지
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    • 제50권2호
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    • pp.161-165
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    • 2012
  • 호박벌 유래 디펜신의 전체 아미노산 서열의 구조 분석 후에 항균활성을 갖는 서열을 선발하였고, 전체 및 펩타이드 길이와 구조적 차이에 대한 종합적인 결과로서 기존에 보고되어진 ${\alpha}$-helix 구조의 펩타이드 보다는 ${\beta}$-sheet의 일부 서열과 ${\alpha}$-helix의 서열이 공존할 때 항균 활성이 보다 뛰어남을 확인하였다. 특히 시스테인-아르기닌 (38C-39R)이 포함되어 있는 펩타이드 서열에서 항균력이 우수하였고, 이는 세포벽에 친화력이 있는 염기성 펩타이드의 특성으로 예상하고 있다.

Enumeration and Recovery of Bacterial Isolates from Ruminants Fed with Different Dietary Regimes and Their Antibacterial Activity

  • Pattnaik, P.;Grover, Sunita;Batish, V.K.
    • Asian-Australasian Journal of Animal Sciences
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    • 제14권6호
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    • pp.811-815
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    • 2001
  • The study evaluated different synthetic and semisynthetic media for maximal recovery of rumen bacteria and expression of their antibacterial activity. Rumen Glucose Cellobiose Agar (RGCA) medium was found to be the best for recovery of rumen bacteria. However, L-10 medium was the best for expression of antibacterial activity of ruminal isolates followed by Easy, M-10, RGCA and M-98-5 medium. The present study recommends the use of L-10 medium as the medium of choice for screening of antibacterial activity of ruminal isolates. Comparative evaluation of bacterial counts on different dietary regimes indicated significant difference between different growth media on a specific diet and between diets on specific growth media within a species. However, there is no overall significant difference between total bacterial counts obtained from rumen liquor of cattle and buffalo with respect to either the feeding regime or growth media. Feeding straw based diet to the animal is the best for high recovery of rumen bacteria.

Syntheses of Resveratrol and its Hydroxylated Derivatives as Radical Scavenger and Tyrosinase Inhibitor

  • Lee, Hyun-Suck;Lee, Byung-Won;Kim, Mi-Ran;Jun, Jong-Gab
    • Bulletin of the Korean Chemical Society
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    • 제31권4호
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    • pp.971-975
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    • 2010
  • Eight hydroxylated stilbene derivatives including resveratrol, desoxyrhapontigenin and piceatannol as potential radical scavenger and tyrosinase inhibitor are synthesized using optimized Wittig-Horner reaction for excellent trans-selectivity in good yields. Antioxidant activity was tested against ABTS radical and tyrosinase inhibitory activity was performed with L-tyrosine as the substrate based on previous procedure with some modification. In general, catecholic stilbenes showed stronger activity against ABTS radical and resorcinolic moiety showed stronger tyrosinase inhibitory activity. Synthetic piceatannol which containing both catecholic and resorcinolic moieties showed the strongest activity in both as ABTS radical scavenger and tyrosinase inhibitor with $IC_{50}$ values of 4.1 and $8.6\;{\mu}M$, respectively.

Synthesis and Structure-activity Relationship of Cytotoxic $5,2^I,5^I$-Trihydroxy-7,8-dimethoxyflavanone Analogues

  • Min, Byung-Sun;Ahn, Byung-Zun;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • 제19권6호
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    • pp.543-550
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    • 1996
  • Analogues of $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone, a naturally-occurring compound, which had been reported to have potent antitumor activity, were synthesized and examined for the cytotoxicity against three cancer cell lines. Among the intermediate chalcones and synthetic 5-hydroxy-7, 8-dimethoxyflavanone analogues, $({\pm})2^{l}, 5^{l}-dibenzyloxy-5, 7, 8-trimethoxyflavanone$ exhibited about 2-8 times stronger activity than $2(S)-5, 2^{l}, 5^{l}$-trihydroxy-7, 8-dimethoxyflavanone against L1210, K562 and A549 cancer cell lines. In the structure-activity relationship, it is suggested that among analogues of 5-hydroxy-7, 8-dimethoxyflavanone, the existence of two oxygenated groups of para-relation at $C-2^{I} and C-5^{I}$ positions on flavanone B-ring, may be necessary to exhibit effective cytotoxic activity.

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