• 제목/요약/키워드: amino acid derivatives

검색결과 214건 처리시간 0.028초

The Synthesis of 1,2-Benzothiazine-3-carboxamidylhydantoin Derivatives and their Antiinflammatory and Analgesic Activities

  • Kwon, Sonn-Kyoung;Park, Myoung-Suk
    • Archives of Pharmacal Research
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    • 제15권3호
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    • pp.251-255
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    • 1992
  • A number of 4-hydroxy-2H (or alkyl)-N-(3-aralkyl-2-thio-1-hydantoinyl)-1, 2-benzothiazine3-carboxamide 1, 1-dioxides were synthesized through the reaction of 4-hydroxy-2H (or alkyl)1, 2-benzothiazine-3-carboxylic methyl ester 1, 1-dioxide and 1-amino-2-thio-3-aralkyl-4-imidazolones in xylene. The compounds synthesized were screened for antinflammatory effect on carrageenin-induced edema in rat and for analgesic effect on acetic acid-induced Writhing syndrome in mice. Most compounds were inhibots of carrageenin-induced rat foot edema and some showed significant antinflammatory activity comparable to that of indomethacin and significant analgesic activity comparable to that of indomethacin and aspirin.

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Synthesis, Characterization and Antimicrobial Activity of Novel Pharmacophores Incorporating Imidazoline-Oxazoline Scaffold

  • Barakat, Assem;Al-Majid, Abdullah Mohammed;Al-Qahatany, Faisal M.;Islam, Mohammad Shahidul;Al-Agamy, Mohamed H.M.
    • Bulletin of the Korean Chemical Society
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    • 제35권2호
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    • pp.562-568
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    • 2014
  • In this work, synthesis, characterization and antimicrobial activity of series of imidazolines-oxazolines scaffolds 5a-f and 10a-d have been investigated. All the imidazolines-oxazolines derivatives were prepared from acid derivatives 1 and 6a-c, and enantiomerically pure (S)-2-amino-3-methyl-1-butanol in four steps with excellent optical purity. The structures of all newly synthesized compounds have been elucidated by $^1H$, $^{13}C$ NMR, GCMS, and IR spectrometry. Their purity was confirmed using elemental analysis. Some newly synthesized compounds were examined to in-vitro antimicrobial activity. Among the prepared products 10d was found to exhibits the most active against all tested bacteria and fungi with minimal inhibitory concentration (MIC) ranged between 21.9 and $42.6{\mu}g/mL$.

옥사졸론 유도체의 합성과 항균성 (Synthesis and Antibacterial Activity of Some Oxazolone Derivatives)

  • Aaglawe M. J.;S. S. Dhule;S. S. Bahekar;P. S. Wakte;D. B. Shinde
    • 대한화학회지
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    • 제47권2호
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    • pp.133-136
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    • 2003
  • 일련의 옥사졸론 유도체들을 (4a-n) 항균제로서 합성하였다. 이 화합물들은 아릴옥시아세틸아미노아세트산을 에탄올, 아세트산 무수물, 아세트산 소듐 존재하에 알데하이드와 반응시켜 합성하였으며 핵자기공명 스펙트럼과 적외선 스펙트럼으로 구조를 확인하였다.

Synthesis and Cytotoxicity Evaluation of Phosphorylated Derivatives of Ribavirin

  • Rao, Valasani Koteswara;Reddy, Sanapalli Subba;Babu, Kilaru Raveendra;Kumar, Kuntrapakam Hema;Ghosh, Sunil Kumar;Raju, Chamarthi Naga
    • 대한화학회지
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    • 제55권6호
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    • pp.952-959
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    • 2011
  • Novel phosphorylated derivatives of ribavirin 5-16 were synthesized by the reaction of 4-nitrophenyl phosphorodichloridate with various amino acid esters in the presence of triethylamine in dry tetrahydrofuran through the intermediates 3. On further reaction of 3 with ribavirin in THF and pyridine in the presence of TEA afforded the title compounds 5-16. Their structures were characterized by IR, $^1H$, $^{13}C$, $^{31}P$ NMR and mass spectral analyses. All the title compounds were found to exhibit potent in vitro anticancer activity against MCF-7 breast cancer cell lines.

화이트바이오텍기반 방향족화합물 개발에 관한 연구동향 (Research Trend about the Development of White Biotech-Based Aromatic Compounds)

  • 이진호
    • 한국미생물·생명공학회지
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    • 제37권4호
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    • pp.306-315
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    • 2009
  • 원유의 고갈, 반복되는 에너지 위기 및 지구온난화 문제에 기인하여 석유 대신 재생가능한 바이오매스를 사용하여 방향족 화학원료를 개발하는 연구가 광범위하게 진행되고 있다. 특히, 바이오테크놀로지를 이용한 포도당으로부터 방향족아미노산 생합성경로 중간대사체 및 그 유도체 합성기술은 벤젠유래 화합물을 포함한 많은 방향족 석유화학원료를 대체할 가능성이 있는 기술들이 개발되고 있다. 본 고는 미생물 대사공학, 생물전환, 화학공정 기술을 이용하여 hydroquinone, catechol, adipic acid, shikimic acid, gallic acid, pyrogallol, vanillin, p-hydroxycinnamic acid, p-hydroxystyrene, p-hydroxybenzoic acid, indigo, indole 3-acetic acid와 같은 방향족화합물을 어떻게 개발하고 있는지를 논하였다. 또한, 경쟁력있는 화이트바이오텍기반 방향족화합물 생산기술을 개발하기 위한 문제점 및 해결방안등을 논했다.

민자주방망이버섯(L. nuda)의 영양성분 분석 (Analysis of Nutritional Components of Lepista nuda)

  • 이양숙;김종봉;신승렬;김남우
    • 한국식품저장유통학회지
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    • 제13권3호
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    • pp.375-381
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    • 2006
  • 민자주방망이버섯의 식품 영양학적 기능적 평가를 위한 기초연구로서 영양 성분의 함량을 조사하였다. 일반성분은 수분 $90.90{\pm}0.09%$, 탄수화물 $4.38{\pm}0.07%$, 조단백질 $3.70{\pm}0.03%$, 조회분 $0.55{\pm}0.04%$ 그리고 조지방이 $0.47{\pm}0.01%$로 분석되었다. 환원당의 함량은 636.17 mg이었고 유리당은 galactose(51.98 mg), trehalose(22.48 mg), maltose(8.48 mg), mannose(7.96 mg), 그리고 arabinose(6.52 mg) 등의 순으로 모두 97.42mg이 함유되어 있었다. 무기질은 K와 Mg가 각각 103.10 mg과 56.01 mg으로 다른 것에 비하여 함유량이 높았다. 민자주방망이버섯의 구성아미노산은 총 310.39 mg이었고, 이 중 필수아미노산이 111.50 mg이었으며, valine(25.40 mg), leucine(22.52 mg), lysine(21.34 mg) 등의 함량이 상대적으로 높았다. 비필수아미노산은 총 198.89 mg이었으며, glutamic acid(60.72 mg), aspartic acid(30.17 mg), alanine(29.72 mg) 등의 함량이 높았다. 유리아미노산은 총 220.86 mg이었으며, 필수아미노산이 36.21 mg으로 isoleucine(21.57 mg), threonine(11.20 mg)의 함량이 높았으며, 비필수아미노산은 184.65 mg으로 glutamic acid(42.78 mg)와 aspartic acid(32.44 mg) 등의 함량이 높았다. 아미노산 유도체의 함량은 총 187.85 mg으로서 hydroxyproline이 121.50 mg으로 가장 높았으며 그 외 citrulline(15.58 mg), ornithine(15.41 mg), $\alpha$-aminoisobutyric acid(11.23 mg) 등의 함량이 높은 것으로 분석되었다.

2-(5-nitro)furylacrylamino acid류의 합성및 항균작용에 관한 연구 (Studies on the synthesis and antibacterial action of 2-(5-nitro) furylacrylamino acid)

  • 고현기
    • 약학회지
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    • 제10권2_3호
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    • pp.15-19
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    • 1966
  • In order to find 2-(5-nitro)furylacrylic acid derivatives possessing antimicrobial activity, nine new 2-(5-nitro)furylacrylamino acids were synthesized which were obtained by the action of 2-(5-nitro)furylacryla chloride on amino acids, such as $_{L}$-phenylalanine, glycine, $_{L}$-isoleucine, $_{L}$-glutamic acid, $_{DL}$-methionine, $_{L}$-threonine, $_{L}$-valine, $_{L}$-tryptophan and $_{DL}$-alanine, according to Schotten-Baumann method. These compounds generally showed a good bactericidal and bacteriostatic activity against Bacillus subtilis but were less effective against staphylococcus aureus, Proteus vulgaris and Escherichia coli. Of the above nine compounds, 2-(5-nitro)furylacryl glycine exhibited a good bactericidal activity.

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7-Aminocephalosporanic acid를 포함하는 Aminophosphonate유도체의 합성 (Synthesis of Aminophosphonate Derivatives Containing 7-Aminocephalosporanic acid)

  • 김상범
    • 공업화학
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    • 제8권4호
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    • pp.700-703
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    • 1997
  • Phthalic anhydride를 출발물질로 halogenation, phosphorylation하여 diethyl phthalimidoalkylphosphonate를 합성하였다. 이 화합물을 chlorination하여 O-ethyl phthalimidoalkylphosphonate을 만든후 diphenylmethyl 7-$\beta$-amino-3-acetoxymethyl-3-cephem-4-carboxylate와 coupling하여 지금까지 알려져 있지 않은 화합물 diphenylmethyl-7-$\beta$-(O-ethylphthalimidomethylphosphony1)-3-acetoxymethyl-3-cephem-4-carboxylate와 diphenylmethyl-7-$\beta$-[O-ethylphthalimidoethylphosphonyl]-3-acetoxymethyl-3-cephem-4-carboxylate를 각각 19%, 43%의 수율로 합성하였다.

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New Fused Quinoxalines : Synthesis and Reactions of Pyrimidothienoquinoxaline and Oxadizolylthienoquinoxalines

  • Moustafa, Osama S.;Badr, Mahmoud Z.A.;El-Emary, Talaat I.
    • Bulletin of the Korean Chemical Society
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    • 제23권4호
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    • pp.567-570
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    • 2002
  • Diazotization of 3-amino-2-ethoxycarbonylthieno[2,3-b]quinoxaline 1 gave the diazonium salt 2 which was reacted with SO2 and N-methylaniline to give sulfamoylquinoxaline derivatives 3-5. Imidazothienoquinoxaline 8 was obtained from the reaction of carboxylic acid hydrazide 6 with nitrous acid and followed by boilling the carboazide 7 in dry xylene. Also, compound 6 react with CH(OEt)3 to give aminopyrimidine 9 which was reacted with arylidene malonodinitrile, furfural and/or dimethoxy-tetrahydrofuran to afford compounds 10, 11 and/or 12 respectively. Refluxing of 6 with CS2 gave oxadiazolylthienoquinoxaline 13, reaction of 13 with hyrazine hydrate, CH(OEt)3, nitrous acid, CS2 and a-halocompounds to give 14-19.

능이[Sarcodon aspratus(Berk, ) S. Ito]에서 분리한 단백질 가수분해 효소의 특성 (Characterization of a Serine Protease from Neungee [Sarcodon aspratus(Berk, ) S. Ito])

  • 엄태붕;유관성;김미경;류재수;손희숙;이태규
    • 한국식품영양과학회지
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    • 제20권1호
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    • pp.35-39
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    • 1991
  • Properties of a protease purified from Neungee[Sarcodon aspratus(Berk, ) S. Ito] have been investigated. The enzyme displays a glycosylated serine protease. The enzyme is able to hydrolyze alanine glycine methionine glutamine and cysteine of N-CBZ and N-t-BOC-L-amino acid derivatibes relatively strongly but splits valine proline and isoleucine derivatives with low affinity which means the enzyme has the broad substrate spectrum toward the amino acids. Interestingly the enzyme was inhibited by bromelain inhibitor. That is the active site environ-ment of the enzyme is believed to be similar to that of bromelain However peptide mapping studies show that the two enzymes have distinct different cleavage sites.

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