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Erlichman. 545 (2–3): 129–133 (2006).

ISSN: 1838-7640

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275 Words


Selected 1,3,4-Oxadiazole Analogs Acting as GSK-3β Inhibitors

11. Song J, McColl J, Camp E, Kennerley N, Mok GF, McCormick D. . Smad1 transcription factor integrates BMP2 and Wnt3a signals in migrating cardiac progenitor cells. 2014;111:7337-42

Selected Analogs of 5-Imino-1,2,4-Thiadiazoles Acting as GSK-3 inhibitors

Two heterocyclic compounds, 5-(4-methoxyphenyl)-1,3,4-oxadiazole-2-thiol (A1) and 5-(4-nitrophenyl)-1,3,4-oxadiazole-2-thiol (A2) were studied as inhibitors of nickel metal corrosion. The kinetic and thermodynamic parameters of corrosion were determined from polarization curves and impedance measurements. It was found that the nickel surface was protected from corrosion when the inhibitor concentration was increased in the corrosive medium. Electrochemical impedance spectroscopy, open circuit potential, and linear scan voltammetry results showed that the corrosion rate of Ni decreased in the presence of inhibitors in a 3.5% NaCl solution, with the inhibition strength in the order A1 > A2. EIS measurements showed that the charge transfer resistances of the nickel surface in 0.16 mM A1 and A2 were 144.2 and 119.3 kΩ cm2 in a 3.5% NaCl solution, respectively. FESEM images showed that the surface was well protected against corrosion when the concentration of inhibitors was increased to 0.3 mM in the corrosive media.

Compound 1: [N-(5-Phenyl-[1, 3, 4] oxadiazol-2-yl)-benzamide]

Compound 2: [2-Chloro-N-[5-(2-chloro-phenyl)-[1,3,4]oxadiazol-2-yl]benzamide]

7. Watkins CC, Sawa A, Pomper MG. Glia and immune cell signaling in bipolar disorder: insights from neuropharmacology and molecular imaging to clinical application. 2014;4:e350

8. Maurer U, Preiss F, Brauns-Schubert P, Schlicher L, Charvet C. GSK-3-at the crossroads of cell death and survival. 2014;127:1369-78


Compound 3: [4-Chloro-N-[5-(4-chloro-phenyl)-[1,3,4] oxadiazol-2-yl]-benzamide]

53. Wang Y, Lam JB, Lam KS, Liu J, Lam MC, Hoo RL. . Adiponectin modulates the glycogen synthase kinase-3beta/beta-catenin signaling pathway and attenuates mammary tumorigenesis of MDA-MB-231 cells in nude mice. 2006;66:11462-70

58. Thomas GM, Frame S, Goedert M, Nathke I, Polakis P, Cohen P. A GSK3-binding peptide from FRAT1 selectively inhibits the GSK3-catalysed phosphorylation of axin and beta-catenin. 1999;458:247-51

Compound 4: [3-Chloro-N-[5-(3-Chloro-phenyl)-[1,3,4] oxadiazole-2yl]benzamide
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  • IQ8 (2-Amino-3-methylimidazo(4,5-f)quinoline) () (1993)

    T1 - Synthesis and antibacterial activity of some new 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives

  • 4,4´-Methylene bis(2-chloroaniline) (MOCA)8 () (1993)

    KW - 1,3,4-oxadiazole

  • 2-Amino-5-(5-nitro-2-furyl)-1,3,4-thiadiazole ()

    KW - 1,3,4-thiadiazole

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MeIQ (2-Amino-3,4-dimethylimidazo(4,5-f)quinoline) () (1993)

97. Cole EL, Shao X, Sherman P, Quesada C, Fawaz MV, Desmond TJ. . Synthesis and evaluation of [11C]PyrATP-1, a novel radiotracer for PET imaging of glycogen synthase kinase-3beta (GSK-3beta). 2014;41:507-12

MeIQx (2-Amino-3,8-dimethylimidazo(4,5-f)quinoxaline) () (1993)

98. Wang M, Gao M, Miller KD, Sledge GW, Hutchins GD, Zheng QH. The first synthesis of [11C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3). 2011;21:245-9

4-(N-Nitrosomethylamino)-1-(3-pyridyl)-1-butanone (NNK) ()

95. Vasdev N, Garcia A, Stableford WT, Young AB, Meyer JH, Houle S. . Synthesis and ex vivo evaluation of carbon-11 labelled N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea ([11C]AR-A014418): a radiolabelled glycogen synthase kinase-3beta specific inhibitor for PET studies. 2005;15:5270-3

PhIP (2-Amino-1-methyl-6-phenylimidazo(4,5-b)pyridine) () (1993)

99. Tolosa E, Litvan I, Hoglinger GU, Burn D, Lees A, Andres MV. . A phase 2 trial of the GSK-3 inhibitor tideglusib in progressive supranuclear palsy. 2014;29:470-8

Trp-P-1 (3-Amino-1,4-dimethyl-5H-pyrido(4,3-b)indole) ()

93. Cole E, Shao X, Fawaz M, Scott P. Radiosynthesis of [11C]PyrATP1, a novel radiotracer targeting the ATP-binding site of GSK-3β. 2014;55:1110

Trp-P-2 (3-Amino-1-methyl-5H-pyrido(4,3-b)indole) ()

103. Zamek-Gliszczynski MJ, Abraham TL, Alberts JJ, Kulanthaivel P, Jackson KA, Chow KH. . Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure. 2013;41:714-26

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