• 제목/요약/키워드: 1-chloro-2

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Antimicrobial and Antineoplastic Tyrosine Metabolites from a Marine Sponge, Aplysina fistularis

  • Goo, Yang-M.
    • Archives of Pharmacal Research
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    • 제8권1호
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    • pp.21-30
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    • 1985
  • Examination of the constituents of a marine sponge, Aplysina fishtularis, indicated that brominated tyrosine metabolites were mainly responsible for antimicrobial and antineoplastic activities. Halogenated tyrosine metabolites, 2, 6-dibromo-(2), 2-bromo-3-chloro-(3) and 2, 6-dibromo-(5), 5-a mino-2-bromo-6-chloro-(6) and 5-amino-2, 6-dich-loro-(7) 4-hydroxy-2-cyclohexenone-4-acetic acid lactams were identified as the major antineoplastic and antimicrobial principles. Many other brominated tyrosine metabolites were also confirmed, but they did not show antimicrobial and antineoplastic activities.

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Synthesis of Substituted Arylazothioxanthones as Potential Schistosomicidal Agents

  • El-Kerdawy, M.M.;El-Emam, A.A.;El-Subbagh, H.I.;Abushanab, E.
    • Archives of Pharmacal Research
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    • 제12권1호
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    • pp.5-7
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    • 1989
  • A series of 1-chloro-4-methyl-6-arylazo-9H-thioxanthen-9-ones were synthesized and schistosomicidal activity evaluated. It was found that, 1-chloro-4-methyl-6-(2-hydroxy-1-naphthylazo)-9H-thioxanthen-9-one possessed a promising activity against Schisto-soma mansoni in mice.

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3-(1'-Benzyl-2'-substituted indol-3'-yl)-1-acrylophenone유도체의 합성에 관한 연구 (A Study on syntheses of 3-(1'-Benzyl-2'-substituted indol-3'yl)-1-acrylophenone)

  • 이기창
    • 한국응용과학기술학회지
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    • 제11권2호
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    • pp.105-111
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    • 1994
  • Intermediates, 1-benzyl-2-substituted-3-carboxaldehyde[I]-[II], were prepared by the reaction of 2-substituted indole-3-carboxaldehyde with benzyl chloride. Indolylacrylophenone derivatives[III]-[X] were prepared from 1-benzyl-2-substituted-3-carboxaldehyde with acetophenone derivatives. They are as follows; 3-(1'-benzylindole-3'-yl)-1acrylophenone [III] 3-(1'-benzylindole-3-yl)-1(p-methoxy)acrylophenone [IV] 3-(1'-benzylindole-3-yl)-1(p-bromo)acrylophenone [V] 3-(1'-benzylindole-3-yl)-1(p-chloro)acrylophenone [VI] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-acrylophenone [VII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-methoxy)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-bromo)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-chloro)acrylophenone [X]

살충성 2-Chloro-1-(2,4,5-trichlorophenyl)vinyldimethylphosphate (Gardona)$^{\(R)}$의 가수분해 반응메카니즘 (Kinetics and Mechanism of Hydrolysis of Insecticidal 2-chloro-1-(2,4,5-trichlorophenyl) vinyldimethylphosphate (Gardona)$^{\(R)}$)

  • 성락도;윤태용;권기성;김태린
    • 대한화학회지
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    • 제34권5호
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    • pp.483-489
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    • 1990
  • 25${\%}$ methanol-수용액 속에서 살충성 2-chloro-l-(2,4,5-trichlorophenyl)-vinyldimethylphosphate(Gardona)의 가수분해 반응을 관찰하였다. 다양한 pH에서의 연구결과는 용매효과(m < 0.4, n < 0.7, |m| ${\ll}$ |l|(화합 S$_N$2 형)), 열역학적 파라미터 (${\{Delta}S^{\neq}$ = -27∼-32 e.u. ${\{Delta}H^{\neq}$ = 13∼18 Kcal/mole), 반응속도(k = k$_A$+k$_B$ [OH$^-$]), 일반염기 촉매 효과 및 가수분해 생성물 분석에 의하여 Gardona의 가수분해 반응이 전이상태와 carbanion 중간체를 포함하는 2분자적(Ad$_{N-E}$) 메카니즘으로 일어남을 암시하고 있다.

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1N-아릴-2-메틸-3-에톡시카르보닐-피리디노 [2,3-f]인돌-4,9-디온 유도체의 합성 (II) (Synthesis of 1N-aryl-2-methyl-3-ethoxycarbonyl-pyridino [2,3-f]indole-4,9-dione derivatives (II))

  • 서명은;박희경
    • 약학회지
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    • 제41권5호
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    • pp.582-587
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    • 1997
  • The 6.7-dichloroquinoline-5,8-dione (I) was reacted with ethyl acetoacetate in the presence of sodium ethoxide to yield 6-(${\alpha}$-acetyl-${\alpha}$-ethoxycarbonyl methyl)-7-chloro-qui noline-5,8-dione(II). When this compound II was reacted with some arylamine (phenyl, p-toluyl, p-fluorophenyl, p-chlorophenyl. p-bromophenyl, p-iodophenyl, p-trifluoromethylphenyl, p-dimethylaminophenyl,indanyl), 1N-aryl-2-methyl-3-ethoxycarbonyl pyridino[2,3-f]-indole-4.9-dione(IIIa-I) were obtained via intramolecular cyclization.

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Synthesis and Characterization of Phosphorescent Platinum and Iridium Complexes of 6-Chloro-3-phenylpyridazine

  • Lee, Sang-Jin;Seok, Kang;Lee, Jae-Sung;Lee, Seung-Hee;Hwang, Kwang-Jin;Kim, Young-Kwan;Kim, Young-Sik
    • Journal of Photoscience
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    • 제10권2호
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    • pp.185-187
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    • 2003
  • The preparation and the photophysics of organometallic Pt(II) and Ir(III) complexes with 6-ch1oro-3-phenylpyridazine (H6Clppdz) are reported. $K_2$PtCl$_4$ and IrCl$_3$ㆍn$H_{2}O$ cleanly cyclometalate with H6Clppdz, forming the corresponding chloro-bridged dimers, (6Clppdz)Pt($\mu$-Cl)$_2$Pt(6Clppdz) and (6Clppdz)$_2$Ir($\mu$-Cl)$_2$Ir(6Clppdz)$_2$ in good yield. These chloro-bridged dimers are cleaved with acetylacetone (Hacac) to give the corresponding monomer, (6Clppdz)Pt(acac) and (6Clppdz)$_2$ Ir(acac), respectively. Both complexes show bright orange luminescence at room temperature and the emission wavelengths are different depending on the metal and the structure of complexes. (6Clppdz)Pt(acac) shows two sharp emission bands in shorter wavelength ($\lambda$$_{em}$=541 and 580 nm), while (6Clppdz)$_2$ Ir(acac) shows a broad emission band in longer wavelength ($\lambda$$_{em}$=615 nm). Strong spinorbit coupling due to the heavy metal atom allows for the formally forbidden mixing of the $^1$MLCT with the $^3$MLCT and $^3$$\pi$-$\pi$$^{*}$ states.

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The antimicrobial Activities of Some 1,4-Naphthalenediones (III)

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • 제16권2호
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    • pp.161-163
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    • 1993
  • In order to evaluate the antimicrobial effect of 2,3-disubstituted-1,4-naphthalenedione derivatives, we synthesized several 2-chloro, 2-bromo and 2-hydroxy-3(substituted)-1, 4-naphthalene-diones (1-25). These derivatives were tested for antifugal and antibacterial activities, in vitro, against Candida albicans 10231 and local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Baciilus subtilis ACTT 6633, Pseudomonas aeruginsa NCTC 10490, Staphylococcus aureus ATCC 6538P, Escherichia coli NIHJ. The MIC values were determined by the two-fold agar dilution/strea method. Among these derivatives, 4, 5 and 6 showed the potent antifungal activities. Also 5 and 6 had the antibacterial activities. 5 with (1,2,4-triazolyl)-amino moirty was the most effective in preventing the growth of fungi, such as Candida albicans, Aspergillus niger and Tricophyton mentagrophytes.

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1N-알킬-2-메틸-3-에톡시카르보닐-피리디노(2,3f)인돌-4,9-디온 유도체 합성 (Synthesis of 1N-alkyl-2-methyl-3-ethoxycarbonyl-pyridino(2,3f)indole-4,9-dione Derivatives)

  • 서명은;박희경
    • 약학회지
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    • 제40권1호
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    • pp.19-24
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    • 1996
  • The 6,7-dichloroquinolone-5,8-dione(I) was reacted with ethyl acetoacetate in the presence of sodium ethoxide to yield 6-(${\alpha}$-acetyl-${\alpha$-ethoxycarbonyl-methyl)-7-chloro-quin oline-5,8-dione(II). When this compound II was reacted with some alkylamine (methylamine, ethylamine, propylamine, isopropylamine, cyclopropylamine, methoxyethylamine, ethanolamine, benzylamine, furfurylamine), 1N-alkyl-2-methyl-3-ethoxycarbonyl-pyridino(2,3f)-indole-4,9-dione(IIIa-i) were obtained via intramolecular cyclization.

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카보닐 탄소원자 친핵 치환반응. 제2보. Methyl chloroformate의 티오 치환제들의 구조와 반응성에 관한 CNDO/2 계산 (Nucleophilic Substitution at a Carbonyl Carbon Atom. Part II. CNDO/2 Studies on Conformation and Reactivity of the Thio-Analogues of the Thio-Analogues of Methyl Chloroformate)

  • 이익춘
    • 대한화학회지
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    • 제16권6호
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    • pp.334-340
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    • 1972
  • 메틸 클로로 티올, 메틸클로로 티오노 및 메틸 클로로 디티오 훠메이트에 대하여 CNDO/2 계산을 실시하였다. 결과로 이들 화합물은 trans형이 안정한 것임을 밝혔다. 또 유황 원자는 산소원자에 비하여 그 고립쌍 전자들을 ${\pi}$-결합 형성에 사용하려는 경향이 적고 티올 훠메이트의 경우는 메틸기의 hyperconjugation에 의하여 안정화됨을 알았다. 가용매 반응성의 순서는 양이온의 안정도와 일치하며 이것은 알려진 $S_N1$형 반응 메카니즘과 부합된다.

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