• Title/Summary/Keyword: 1,3-Diones

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3D-QSAR Analysis on the Photosystem II Inhibition Activity of 6-Bromobenzo[4,5]imidazo[$1,2{\alpha}$]pyridin-8,9-dione Analogues (6-Bromobenzo[4,5]imidazo[$1,2{\alpha}$pyridin-8,9-dione 유도체들의 Photosystem II 저해활성에 관한 3D-QSAR 분석)

  • Kim, Se-Gon;Cho, Yun-Gi;Hwang, Tae-Yeon;Sung, Nack-Do
    • The Korean Journal of Pesticide Science
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    • v.12 no.1
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    • pp.18-23
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    • 2008
  • 3D-QSAR on the inhibitory activities of 6-bromobenzo-[4,5]imidazo[$1,2{\alpha}$]-pyridin-8,9-diones analogues as substrate molecule were studied quantitatively using CoMFA and CoMSIA methods. The statistical values of CoMFA model was better predictability and fitness than CoMSIA model. The inhibitory activities according to the optimized CoMFA 2 model were dependent on the steric field (90.4%). From the CoMFA contour maps, it is found that the branched side chain as R-group will be directly attached to the carbon atom (ipso carbon) of substituent, the inhibitory activities had expected to increase. The positive charge favor groups were placed in the position between imidazol ring and pyridine ring, the inhibitory activities would increase. And if the groups of liner type will be substituted, hydrophilic favor group would raise inhibitory activities.

Regioselective Substitution of 6,7-DichloroQuinoline-5.8-dione: Synthesis, Cytotoxicity, and X-ray crystal stucture of 4a,10.11- Triazabenzo [3.2-a] fluorene-5,6-diones

  • Lee, Hyun-Jung;Park, So-Young;Lee, Chong-Ock;Suh, Myung-Eun
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.342.1-342.1
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    • 2002
  • 6.7-Dicholroquinoline-5.8-dione reacted with 2-aminopyridine derivatives, Out of the four possible products which could be achieved in this reaction. condensation and rearrangement product. 4a.10.11-triazabenzo[3.2-a] fluorine-5.6-dione was obtained as major product. The definite structure was identified with X-ray crystallographic study. (omitted)

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Synthesis of Some Quinoxaline Derivatives Containing Indoline-2,3-dione or Thiazolidinone Residue as Potential Antimicrobial Agents

  • Gendy, Adel-A. El;Meligie, Salwa-El;Afaf-K. El-Ansary;Aly-M. Anmedy
    • Archives of Pharmacal Research
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    • v.18 no.1
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    • pp.44-47
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    • 1995
  • The synthesis of osme quinoxaline derivatives containing indoline-2, 3-dione or thiazolidlinone residue is described. The synthesized derivatives were sureened in vitro for their growth inhibitory activity against six species of bacteria, viz. Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Serratia marcescens and Mycobacterium semegmatils. Most of the compounds exhibited antimicrobial activity especially those having indoline-2, 3-dione moiety.

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Novel Conversion of 2-(4-Dimethylaminoaryl)-1,4-diphenylbutane-l,4-diones into 3-(4- Dimethylaminoaryl)-l-phenylpropenones via Debenzoylation and Oxidation

  • Kim, Sung-Sik;Chang, Ji-Ae;Kim, Ae-Rhan;Cho, Kyung-Won;Park, Sang-Kyu
    • Journal of Photoscience
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    • v.12 no.2
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    • pp.109-111
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    • 2005
  • It was found that 1,4-diketones such as 1,4-diphenyl-l,4-butanediones containing N,N-dimethylaminophenyl (pDPB) and N,N-dimethylaminonaphthyl (nDPB) at C2 are converted into 3-(4-dimethylaminoaryl)-1-phenylpropan-lones (pPPA and nPPA) by treatment with $Ca(OH)_2$ in methanol, which was easily oxidized to enone, i.e., 3-(4-dimethylaminophenyl)-l-phenylpropenones (pPPE and nPPE), when treated with 2,3-dichloro-5,6-dicyano-l,4-benzoquinone (DDQ) in dichloromethane.

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Reactions of Some Furan-3-ones with 2,3-Diaminopyridine and its Derivatives

  • Sacmacl, Mustafa;Bolukbasl, Hilal;Sahin, Ertan
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.90-94
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    • 2012
  • The furan-2-ylidene acetates (3a-d), obtained from the furan-2,3-diones (1a-b) and methyl/ethyl (triphenylphosphoranylidene)-acetates (2a-b), were converted via the Michael type reactions with 2,3-diaminopyridine and its derivatives (4a-c) into the corresponding pyrrol-2-ylidene-acetates (5a-j) in moderate yields (45-94%). Structures of these compounds were determined by the IR, NMR, elemental analysis, and X-ray diffraction method.

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

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.16 no.2
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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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Synthesis of a New Diels-Alder Quinone Adduct and Its Use in Preparing Thiazolo- and Oxazoloquinolines

  • Hammam, A.S.;Youssef, M.S.K.;Radwan, Sh.M.;Abdel-Rahman, M.A.
    • Bulletin of the Korean Chemical Society
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    • v.25 no.6
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    • pp.779-785
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    • 2004
  • Syn (or anti) cinnamaldehydeoxime (1a, b) undergoes Diels-Alder addition to tetrabromo-p-benzoquinone (2)in dry xylene in 1 : 1 and 2 : 1 molar ratios to give the mono- and diadducts 3 and 4a, b respectively. The reaction of 3 with thioamides in ethanol gave thiazoloquinoline diones 6a-d, whereas with acid amides in ethylene glycol, it gave oxazoloquinolinediones 12a-f.