• Title/Summary/Keyword: Oxadiazole

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1,3,4-Oxadiazole-2(3H)-thione as a New Scaffold for Pim Kinase Inhibitors

  • Lee, Ah Yeon;Hong, Victor Sukbong;Lee, Jinho
    • Quantitative Bio-Science
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    • v.37 no.2
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    • pp.113-124
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    • 2018
  • Pim kinases are important targets for cancer therapies because they are mainly responsible for cancer metastasis and overall therapeutic treatment responses. Because of their unusual structural feature in the hinge region of the ATP-binding site, new binding motifs have been discovered and used for the development of Pim kinases inhibitors. The results of a screening of 5-membered heteroaromatic compounds and the effects of structural modifications on the inhibition of Pim kinases' activities showed the potential scaffold for Pim inhibitors. 1,3,4-Oxadiazole-2(3H)-thione was found as a new scaffold for Pim kinase inhibitors.

Synthesis, Antinicrobial and Molluscicidal Activities of New Benzimidazole Derivatives

  • Nofal, Z.M.;Fanmy, H.H.;Mohamed, H.S.
    • Archives of Pharmacal Research
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    • v.25 no.1
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    • pp.28-38
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    • 2002
  • A series of Schiff's benzimidazole bases, thiosemicarbazides were synthesized, azole ring systems as 1,3,4-triazole, 1,3,4-oxadiazole were prepared. 1-Methylbenzimidazole incorporated to substituted dithio-carbamate, thiophenol, diethylamine via acetamido group were synthesized. A series of pyrimidinobenzimidazoles, triazinobenz-imidazoles, and 2-(acetonylamino)-1-methyl-benzimidazole were prepared. The antimicrobial and molluscicidal activities of some newly prepared compounds were carried out.

Synthesis and Properties of Liquid Crystalline Y-shaped Molecules Containing 1,3,4-Oxadiazole

  • Kwon, Eun-Kyoung;Choi, E-Joon
    • 한국정보디스플레이학회:학술대회논문집
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    • 2007.08a
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    • pp.542-544
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    • 2007
  • New liquid crystalline Y-shaped molecules containing 1,3,4-oxadizoles have been synthesized with variation of terminal groups (R = H, $OCH_3$ or $OC_8H_{17}$). The structures of obtained compounds were identified by FT/IR and NMR spectrometry, and their thermal and liquid crystalline properties were investigated by DSC and polarizing optical microscope.

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Yellow Light-Emitting Poly(p-phenylenevinylene) Derivative with Balanced Charge Injection Property

  • Kim, Joo-Hyun;Lee, Hoo-Sung
    • Bulletin of the Korean Chemical Society
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    • v.25 no.5
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    • pp.652-656
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    • 2004
  • A new luminescent polymer, poly{1,4-phenylene-1,2-ethenediyl-2'-[2"-(4'"-octyloxyphenyl)-(5"-yl)-1",3",4"-oxadiazole]-1,4-phenylene-1,2-ethenediyl-2,5-bis-dodecyloxy-1,4-phenylene-1,2-ethenediyl} (Oxd-PPV), was synthesized by the Heck coupling reaction. Electron withdrawing pendant, conjugated 1,3,4-oxadiazole (Oxd), is on the vinylene unit. The band gap of the polymer figured out from the UV-visible spectrum was 2.23 eV and the polymer film shows bright yellow emission maximum at 552 nm. The electroluminescence (EL) maximum of double layer structured device (ITO/PEDOT:PSS/Oxd-PPV/Al) appeared at 553 nm. Relative PL quantum yield of Oxd-PPV film is 3.6 times higher than that of MEH-PPV film. The HOMO and LUMO energy levels of Oxd-PPV figured out from the cyclic voltammogram and the UV-visible spectrum are -5.32 and -3.09 eV, respectively, so that more balanced hole and electron injection efficiency can be expected compared to MEH-PPV. A double layer EL of Oxd-PPV has an maximum efficiency of 0.15 cd/A and maximum brightness of 464 cd/$m^2$.

Synthesis of Some 2-Amino-5-Substituted-1,3,4-Oxadiazoles Through the Electrooxidation of Semicarbazone (세미카바존의 전기적 산화에 의한 2-Amino-5-Substituted-1,3,4-Oxadiazoles 합성)

  • Kumar, Sanjeev
    • Journal of the Korean Chemical Society
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    • v.53 no.2
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    • pp.159-165
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    • 2009
  • The synthesis of 2-amino-5-substituted-1,3,4-oxadiazoles 4 were carried out from the electrooxidation of semicarbazone 3 at the platinum electrode under controlled potential electrolysis in an undivided cell. This is an environmentally benign method in the field of synthetic organic chemistry. The non-aqueous solvents acetic acid and acetonitrile and a supporting electrolyte lithium perchlorate were used for the electrolysis in the electrooxidation. The products were structurally charecterised by IR, $^1H$-NMR, $^{13}C$-NMR and elemental analysis.

Synthesis and Antibacterial Evaluation of Some Novel 1,3,4-oxadiazol Derivatives Incorporated with Quinoline Moiety (Quinoline moiety를 가지고 있는 1,3,4-oxadiazol 유도체의 합성 및 항균활성)

  • Mandhane, Priyanka G.;Joshi, Ratnadeep S.;Khan, Wajid;Gill, Charansingh H.
    • Journal of the Korean Chemical Society
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    • v.55 no.4
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    • pp.656-661
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    • 2011
  • 5-(3,4,5-Triethoxyphenyl)-1,3,4-oxadiazole-2-thiol 6 on treatment with substituted 3-(bromomethyl)-2-chloroquinoline or 2-(p-tolyloxy)-3-(bromomethyl)quinoline 4a-j afforded the corresponding 3-((5-(3,4,5-triethoxyphenyl)-1,3,4-oxadiazol-2-ylthio)methyl)-2-chloroquinoline or 3-((5-(3,4,5-triethoxyphenyl)-1,3,4-oxadiazol-2-ylthio)methyl)-2-(p-tolyloxy)quinoline 7a-j, in the presence of $K_2CO_3$ and DMF under stirring at ambient temperature. All the synthesized compounds were further screened for their antibacterial activities. Some of our compounds showed excellent antibacterial activities against test organisms and reference standard.

A study on the electrophotographic properties of ${\tau}-H_2P_c$/oxadiazole photoreceptor (III) (${\tau}-H_2P_c$/oxadiazole 유기이층막의 감광특성 연구 (III))

  • Oh, S.H.;Park, J.K.;Shin, T.H.;Kim, Y.J.;Park, G.B.;Lee, D.C.
    • Proceedings of the KIEE Conference
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    • 1994.07b
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    • pp.1397-1399
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    • 1994
  • The purpose of this study is to measure the electrophotographic characteristics of double-layered organic photoreceptor made by dip-coating method, and to evaluate an application for the laser beam printer drum. From the result, electrophotographic characteristics of the photoreceptor were depend on the thickness of the CTL and the initial surface potential.

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Synthesis and Evaluation of the Analgesic and Antiinflammatory Activities of O-Substituted Salicylamides

  • Fahmy, H.H.;El-Eraky, W.
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.171-179
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    • 2001
  • The present investigation deals with the synthesis of some new salicylamidoacetyl sulfonamides 3a,b, salicylamido ethylacetate 4, salicylamido acetic acid hydrazide 5, which is considered as the key intermediate for the synthesis of several series of new compounds such as salicylamido pyrazol 6 and pyrazolone 1. N-imido-derivatives 9, 10, 11, thiadiazole 13, oxadiazole 14, 15, Schiffs bases 16a-f. Cyclocondensation of Schiffs bases with thioglycolic acid gave thiazolidinone 18a-c while with acetylchloride afforded azitidinones 19a-c and with acetic anhydride gave 1,4-benzoxazepine-3,5-dione. Some of the compounds were tested for their analgesic and antiinflammatory activities as well as ulcerogenic effects. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered .

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Design and Synthesis of New Fluorene-Based Blue Light Emitting Polymer Containing Electron Donating Alkoxy Groups and Electron Withdrawing Oxadiazole

  • Kim, Yun-Hi;Park, Sung-Jin;Park, Jong-Won;Kim, Jin-Hak;Kwon, Soon-Ki
    • Macromolecular Research
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    • v.15 no.3
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    • pp.216-220
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    • 2007
  • A new polyfluorene-based copolymer having 2-ethylhexyloxy-5-methoxy-l,4-phenylene as an electron donating group and 2,5-diphenyl-oxadiazole as an electron withdrawing group was synthesized by the Suzuki coupling reaction. The obtained copolymer was characterized by $^1H-NMR,\;^{13}C-NMR$, and IR-spectroscopy. The weight average molecular weight ($M_w$) of the obtained polymer was 18,600 with a polydispersity index of 1.5. The maximum photoluminescence of the solution and film of the polymer was observed at 453 nm and 456 nm, respectively. A double-layer device with the configuration, ITO/PEDOT/copolymer/Al, emitted blue light at 460 nm.