• 제목/요약/키워드: Benzoquinoline

검색결과 5건 처리시간 0.015초

Synthesis and Evaluation of Benzoquinolinone Derivatives as SARS-CoV 3CL Protease Inhibitors

  • Ahn, Tae-Young;Kuo, Chih-Jung;Liu, Hun-Ge;Ha, Deok-Chan;Liang, Po-Huang;Jung, Young-Sik
    • Bulletin of the Korean Chemical Society
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    • 제31권1호
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    • pp.87-91
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    • 2010
  • For the discovery of new antivirals against Severe Acute Respiratory Syndrome-coronavirus (SARS-CoV), we prepared and evaluated several benzoquinoline compounds as its 3C-like protease (3CLpro) inhibitors. Based on the computer modeling study that each of the two rigid benzoquinolinone and N-phenoltetrazole moieties of the compound 1 is bound to the S1 and S2 sites, respectively, of the SARS protease by forming H-bonds and hydrophobic interactions, we designed and synthesized alkylated benzoquinolines at both the sites of the hydroxyl groups. We found that the compound 2a showed five times higher inhibiting activity against the 3CLpro compared to the compound 1.

식물 특정효소저해제의 생물활성 조사에 의한 신규제초제 작용점 탐색 (Searching of Possible Target Enzymes for Herbicide Development using Commercial Plant-Specific Inhibitors)

  • 황인택;최정섭;박상희;이관휘;이병회;홍경식;조광연
    • 농약과학회지
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    • 제5권1호
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    • pp.36-45
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    • 2001
  • 본 연구는 새로운 제초제 후보물질을 탐색하기 위하여 식물특이적 효소 저해제로 알려진 107개 기존 화합물에 대하여 생물활성을 조사하였다. Germination test, seedling assay, wheat leaf disc assay, cyanobacteria assay, whole plant assay를 통하여 15종의 저해제를 선발하였고 이들은 34종 효소를 저해하는 것으로 확인되었다. 이들 화합물 중에서 phenylhydrazine, purine, o-phenanthroline, oleylamine, 7,8-benzoquinoline, aminooxyacetic acid, dicyclohexylcarbodiimide 등은 성체를 이용한 온실 실험에서 높은 제초활성을 나타내었다. 7,8-benzoquinone, 8-hydroxyquinoline, 2,2'-dipyridyl 및 o-phenanthroline 등은 피, 벼, 토마토의 발아를 $1.25{\sim}5{\mu}M$의 농도에서도 억제하였다. 7,8-benzoquinoline, cyanuric fluoride, 4-methylpyrazole, tranylcypromine, oleylamine과 trifluoperazine 등은 $30{\sim}100{\mu}M$ 농도에서 cyanobacteria의 생육을 저해하였다. Dicyclohexyl carbodiimide와 chlorpromazine은 $100{\mu}M$ 농도에서 wheat leaf disc의 백화현상을 유기시켰다. 이상과 같이 생물학적 활성을 갖는 식물 특이적 효소저해제들은 신규제초제 후보물질을 선발하기 위한 새로운 대상효소로 이용될 수 있을 것으로 생각된다.

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Iridium(Ⅲ) Insertion into an Aromatic C-H Bond and Si-H Bond

  • Yang Nam Keun;Chung Dae-Eun;Ko Jaejung;Kang Sang Ook
    • Bulletin of the Korean Chemical Society
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    • 제13권6호
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    • pp.627-631
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    • 1992
  • The dihydrido iridium(Ⅲ) complex [$Ir(PPh_3)_2H_2(ac)_2$]$BF_4$ (ac=acetone) reacts with 2-phenylpyridine and 7,8-benzoquinoline to yield the C-H activated complexes [$Ir(PPh_3)_2$H(ac)(L)]$BF_4$ (L= phenylpyridine; 7,8-benzoquioline). The dihydrido iridium(Ⅲ) complex [$Ir(PPh_3)_2H_2(ac)_2$]$BF_4$ also reacts with triaklysilane via an oxidative addition reaction to yield the trihydrido iridium complexes [$Ir(PPh_3)_2H_3SiR_3$]$BF_4$ (R =Et and Ph). The structual configuration was studied by conventional spectroscopy.

Rhodium(I) Complexes of 1,1$^\prime$-Bis(diphenylphosphino)-ferrocene as Efficient Catalysts in Regioselective Hydrogenation of Polynuclear Heteroaromatic Compounds

  • Kim, Tae-Jeong;Lee, Kyu-Chul
    • Bulletin of the Korean Chemical Society
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    • 제10권3호
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    • pp.279-282
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    • 1989
  • Two rhodium(I) complexes of the types [Rh(BPPF)(NBD)]$ClO_4$ (10) and [Rh(BPPF)$Cl]_2$ (11) (BPPF = 1,1'-bis(diphenylphosphino)-ferrocene) have been prepared and investigated as catalysts for the regioselective hydrogenation of polynuclear heteroaromatic nitrogen and sulfur compounds such as quinoline (1), acridine (2), phenanthridine (3), 7,8-benzoquinoline (4), benzothiophene (5), isoquinoline (6), indole (7), pyridine (8), and thiophene (9). Both complexes 10 and 11, except for the cases of indole (7) and mononuclear heteroaromatics 8-9, are very efficient in the selective reduction under quite mild hydrogenation conditions to give the corresponding saturated nitrogen and sulfur heterocyclic analogues of 1-6 in fast conversion rates and in excellent yields. Relative rate studies revealed that the reduction depends significantly on the steric and electronic effects of the substrates. Of the two complexes 10-11, the dimeric species 11 gives faster reaction rates in all cases studied.

감초 추출물의 약리적 특성 및 분석 (A Study on the Pharmacetical Characteristics & Analysis of Glycyrrhizin Extract)

  • 성기천
    • 한국응용과학기술학회지
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    • 제23권3호
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    • pp.215-222
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    • 2006
  • From experiment results on pharmacetical characteristics and analysis of Glycyrrhizin extract, some conclusions are obtained as follows. From results on extract experiment of Glycyrrhizin, it appeared about 8%-extraction ratio as semi-solid state, and after dried in freezing from Glycyrrhizin extract of semi-solid state, it obtained about 70%-Glycyrrhizin extract as solid state of yellow gold color. From results on antimicrobial experiment of Glycyrrhizin extract, number of S-typhimurium and Fungus in microbe decreased more and more according to time passage. This phenomenon shows that Glycyrrhizin extract keeps antimicrobial effect. From results on antioxidation experiment of Glycyrrhizin extract, DPPH scavenging activity of free radical shows that Glycyrrhizin extract appears more remarkable reduction ability than reference samples. This phenomenon means that antioxidation of Glycyrrhizin extract appears higher than Vitamin-C and BHA. From results on instrument analysis, the fatty and aromatic components of 2-pentanone, cyclohexasiloxane, tetrasiloxane, benzoquinoline-2-carboxylic acid etcs from Glycyrrhizin extract was detected with GC/MS and inorganic components of Ca, Mg, Ti, Zn, Fe etcs from Glycyrrhizin extract was detected with ICP/OES.