• Title/Summary/Keyword: Pyrrolo[3

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( Syntheses of Improved Polymer/Organic Materials for Electroluminescence(EL) Device and Electro-Optical Characteristics I. Properties of Dye Doped Organic EL Device (고기능 EL소자용 고분자/유기 재료의 합성 및 전기 광학적 특성 I. 색소 도핑에 의한 EL소자의 특성)

  • 김성훈
    • Journal of the Korean Graphic Arts Communication Society
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    • v.13 no.2
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    • pp.33-45
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    • 1995
  • 1, 4-Diketo-3, 6-diphenyl-pyrrolo-[3, 4c]-pyrrole(abbriviated DPP) is a new heterocyclic pigment of red color whose chlorinated derivative is now on the market. DDP was synthesized from benzonitrile and diethylsuccinate. Pariser-parr-pople(PPP) molecular orbital calculations have been carried out on the DPP in other to study spectroscopically the DPP chromophore on deprotonation.

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Synthesis of Tetracyclic Pyrido[2,3-b]azepine Derivatives as Analogues of Mirtazapine via N-Acyliminium Ion Cyclization

  • Lee, Jae-Yeol;Bang, Sung-Hun;Lee, Sook-Ja;Song, Yun-Seon;Jin, Chang-Bae;Park, Ho-Koon;Lee, Yong-Sup
    • Bulletin of the Korean Chemical Society
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    • v.23 no.11
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    • pp.1623-1628
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    • 2002
  • Tetracyclic pyrido[2,3-b]azepine derivatives 4a-d and 4f as analogues of mirtazapine were synthesized via N-acyliminium ion cyclization by using aromatic rings such as benzene and thiophene ring as a ${\pi}-nucleophile$, and evaluated for the binding affinity for ${\alpha}2-adrenoceptor$. Among tested compounds, 2,3,9,13b-tetrahydro-1H-benzo[f]pyrrolo[2,1-a]pyrido[2,3-c]azepine (4a) was the most potent (Ki = 0.26 ${\mu}M)$ but showed about 3-fold less binding affinity than mirtazapine (Ki = 0.08 ${\mu}M)$ for a2-adrenoceptor.

Modeling Aided Lead Design of FAK Inhibitors

  • Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.4 no.4
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    • pp.266-272
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    • 2011
  • Focal adhesion kinase (FAK) is a potential target for the treatment of primary cancers as well as prevention of tumor metastasis. To understand the structural and chemical features of FAK inhibitors, we report comparative molecular field analysis (CoMFA) for the series of 7H-pyrrolo(2,3-d)pyrimidines. The CoMFA models showed good correlation between the actual and predicted values for training set molecules. Our results indicated the ligand-based alignment has produced better statistical results for CoMFA ($q^2$ = 0.505, $r^2$ = 0.950). Both models were validated using test set compounds, and gave good predictive values of 0.537. The statistical parameters from the generated 3D-QSAR models were indicated that the data are well fitted and have high predictive ability. The contour map from 3D-QSAR models explains nicely the structure-activity relationships of FAK inhibitors and our results would give proper guidelines to further enhance the activity of novel inhibitors.

Synthesis and Potent Anti-leukemic Activity of Novel 5'-Norcarbocyclic C-nucleoside Phosphonic Acids

  • Kim, Seyeon;Kim, Eunae;Oh, Chang-Hyun;Yoo, Kyung Ho;Hong, Joon Hee
    • Bulletin of the Korean Chemical Society
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    • v.35 no.12
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    • pp.3502-3508
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    • 2014
  • The first synthetic route to 5'-norcarbocyclic C-nucleoside [7-oxa-7,9-dideazadenosine (furo[3,2-d]pyrimidine) and 9-deazaadenosine (pyrrolo[3,2-d]pyrimidine)] phosphonic acids from commercially available 1,3-dihydroxy cyclopentane was described. The key C-C bond formation from sugar to base precursor was performed using Knoevenagel-type condensation from a ketone derivative. Synthesized C-nucleoside phosphonic acids were tested for anti-HIV activity as well as anti-leukemic activity. Compound 26 showed significant anti-leukemic activity.

Synthesis and Cycloaddition Reaction of C-(2-naphthoyl)-N-arylmethanohydrazonoylpyridinium Bromides

  • Hassaneen, Hamdi M.;Shawali, Ahmad S.;Elwan, Nehal M.;Abounada, Nada M.;Algharib, Mohammed S.
    • Archives of Pharmacal Research
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    • v.15 no.4
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    • pp.292-297
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    • 1992
  • Coupling of naphthacylpyridinium bromide 2 [1-(2-naphthyl) ethanone-2-pyridinium bromide] with N-nitrosoacetarylamides afforded C-(2-naphthoyl)-N-arylmethanohydrazonoylpyridinium bromides 3A-C. Treatment of 3A-C with base afforded the corresponding tetrazines 6A-C. Cycloaddition of nitrilimines 5A-C to N-arylmaleimides, acrylonitrile, ethyl acrylate, acrylamide, fumaronitrile, $\alpha$-cyanocinnamonitriles, ethyl $\alpha$-cyano-p-nitrocinnamates and $\alpha$-cyano-p-nitrocinnamamide afforded the corresponding cycloadducts 7-14, respectively. The cycloadducts 11-14 undergo a facile thermal elimination of hydrogen cyanide to give the corresponding pyrazoles 18-21 respectively.

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Synthesis and Cycloaddition Reactions of N-Aryl-2-furohydrazonyl Chlorides

  • S, Shawali-Ahmad;M, Hassaneen-Hamdi;A, Ibrahim-Hossin
    • Archives of Pharmacal Research
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    • v.13 no.2
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    • pp.126-131
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    • 1990
  • The novel N-phenyl-2-furohydrazonyl chloride 4A and its p-nitro analog 4B have been prepared and identified. The cycloaddition reactions of nitrilimines 5A and 5B, derived by base catalyzed dehydrochlorination of 4A and 4B respectively, to a variety of dipolarophiles were investigated. The results showed that 4A and 4B are usuful precursors for synthesis of differently substituted 3-(2-furyl)-2-pyrazoline derivatives and their pyrazoles and analogs.

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New Synthesis of Chromonopyrroloimidazolinones and Arylidene Thioxoimidazolinones -Study of their antimicrobial activities-

  • Abdel Aziz, Mahfouz A.;Riad, Bahia Y.;Shalaby, A.M.
    • Archives of Pharmacal Research
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    • v.12 no.1
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    • pp.12-16
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    • 1989
  • 6-Formyl-5-methoxy-2-methyl chromone derivatives condensed with 2-thiox-4-imidazolinone derivatives to form the corresponding '10-methoxy-7-methyl-3-thioxo-chromone[6,7-b]pyrrolo[1,2-a-]-imidazolin-1-one derivatives (IIIa-f) or the 5-arvlidene-2-thioxo-4-imidazolinone derivatives(IVa-f). The activity of the NH in the imidazol moiety of (IIIa) was confirmed by formation of the Mannich bases (Va, b). Moreover, alkylation of (IIIa) was undertaken to give the alkylmercapto derivatives (VIa, b). The antimicrobial activities of compounds IIIb-e, IVa, IVe were studied.

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