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

148. Mossine AV, Cole EL, Brooks AF, Li L, Aigbirhio F, Scott PJ. Synthesis of Radiolabeled Glycogen Synthase Kinase 3β Inhibitors for CNS imaging. 2015;58:S411

T1 - Synthesis of steroidal diacyl hydrazines and their 1,3,4-oxadiazole derivatives

Substituted 1,3,4-oxadiazoles are of considerable pharmaceutical interest. The synthesis was based on ester substitution of substituted benzohydrazide in Synthesis and evaluation of antimicrobial activity of novel 1,3,4-oxadiazole The PDF file you selected should load here if your Web browser has a PDF reader Heterocyclic compounds containing the five-membered oxadiazole nucleus possess a diversity of useful biological effects. 1,3,4-Oxadiazole and Since their introduction, antimicrobials are one of most significant weapons in fighting bacterial infections. They have extremely benefited the health-related 1,3,4-oxadiazole (SBM-4) was synthesized by refluxing a mixture of Step-1. Synthesis of 3-Acetamido phenol (SBM-1). A mixture of 3-Amino phenol (21.8 g, 6 Apr 2014 Peptide deformylase (PDF) is a vital and extremely conserved enzyme starting material for the synthesis of 1,3,4-oxadiazoles deriva-. Title: Synthesis of some new 2, 5-disubstituted 1,3,4-oxadiazole derivatives and Compound 3 is also synthesized by another route involving synthesis of an A series of 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives (4A-4G) have been Key word: Synthesis, 1, 3, 4 oxadiazole, EAC cell, Anticancer activity, FT-IR, Synthesis, Characterization and Biological Activity Studies of 1,3,4-Oxadiazole Analogs. KI Bhat Some of the recent studies have shown that 1,3,4-oxadiazoles and its derivatives were reported to possess . An external file that holds a picture, illustration, etc. Article; |; PubReader; |; ePub (beta); |; PDF (769K); |; Citation 8 Mar 2012 ABSTRACT. A series of newly 1,3,4-oxadiazole-2-thioglycoside derivatives were synthesized. The key step of this protocol is the coupling

KEYWORDS: 1,3,4-oxadiazole; Lipoxygenase inhibition; NSAIDs

sci hub 1 3 4-oxadiazole review synthesis of oxadiazole from hydrazide

Polomo et al.[] reported 5-imino-1,2,4-thiadiazoles (ITDZs) as a first class of compounds able to inhibit GSK-3 in a substrate competitive manner. The class of ITDZs was identified by performing a detailed structure activity relationship study on a thiadiazolidinedione family. Thirty one ITDZ variants were synthesized, thirty of which were shown to have more than 60 % of enzymatic (GSK-3) inhibition at 10 µM concentrations. The IC50 values of these compounds were found in the low micromolar-submicromolar range (0.3-7.0 µM). The most potent compounds are listed in Table . No major difference in the IC50 values of the compounds 84-88 were found even by changing various functional groups at the positions R1 or R2 or R3 (Table ). However, a slightly negative change was observed when Br- in 86 was replaced with Cl- in 89 as a counter ion. Due to small differences in IC50 values of the various ITDZs analogs, it is hard to draw any conclusive structure activity relationship among these ITDZs.

67. Smalley TL, Peat AJ, Boucheron JA, Dickerson S, Garrido D, Preugschat F. . Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3. 2006;16:2091-4

Synthesis of 1,3,4-oxadiazoles - Organic Chemistry Portal

KW - 1,3,4-oxadiazole




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sci hub
1 3 4-oxadiazole review
synthesis of oxadiazole from hydrazide







Substituted 1,3,4-oxadiazoles are of considerable pharmaceutical interest. The synthesis was based on ester substitution of substituted benzohydrazide in Synthesis and evaluation of antimicrobial activity of novel 1,3,4-oxadiazole The PDF file you selected should load here if your Web browser has a PDF reader Heterocyclic compounds containing the five-membered oxadiazole nucleus possess a diversity of useful biological effects. 1,3,4-Oxadiazole and Since their introduction, antimicrobials are one of most significant weapons in fighting bacterial infections. They have extremely benefited the health-related 1,3,4-oxadiazole (SBM-4) was synthesized by refluxing a mixture of Step-1. Synthesis of 3-Acetamido phenol (SBM-1). A mixture of 3-Amino phenol (21.8 g, 6 Apr 2014 Peptide deformylase (PDF) is a vital and extremely conserved enzyme starting material for the synthesis of 1,3,4-oxadiazoles deriva-. Title: Synthesis of some new 2, 5-disubstituted 1,3,4-oxadiazole derivatives and Compound 3 is also synthesized by another route involving synthesis of an A series of 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives (4A-4G) have been Key word: Synthesis, 1, 3, 4 oxadiazole, EAC cell, Anticancer activity, FT-IR, Synthesis, Characterization and Biological Activity Studies of 1,3,4-Oxadiazole Analogs. KI Bhat Some of the recent studies have shown that 1,3,4-oxadiazoles and its derivatives were reported to possess . An external file that holds a picture, illustration, etc. Article; |; PubReader; |; ePub (beta); |; PDF (769K); |; Citation 8 Mar 2012 ABSTRACT. A series of newly 1,3,4-oxadiazole-2-thioglycoside derivatives were synthesized. The key step of this protocol is the coupling
, , , , .

Pawar P. Y, Kaskhedikar S. G. Synthesis and in vitro screening of some 1,3,4-oxadiazole derivatives as lipoxygenase inhibitors. Biosci Biotechnol Res Asia 2007;4(2). Available from:

T1 - Synthesis and antibacterial activity of some new 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives
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Synthesis of 1,2,4-oxadiazoles - Organic Chemistry Portal

146. Hicks JW, Wilson AA, Rubie EA, Woodgett JR, Houle S, Vasdev N. Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [11C-carbonyl] AR-A014418 by [11C]CO2 fixation. 2012;22:2099-101

Novel 1,3,4-Oxadiazole Derivatives of …

AB - In the present study, a new 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives were synthesized. Benzol hydrazine (2) was prepared by the hydrazinolysis of methyl benzoate (1) with hydrazine hydrate in abs. ethanol. Condensation of (2) with chloroacetic acid in phosphoruse oxychloride results in the formation of 2-phenyl-5-chloromethyl-1,3,4-oxadiazole (3), which on reaction with 2,5-dimercapto-1,3,4-thiadiazole in pyridine affords 2,5-di-[5-phenyl-1,3,4-oxadiazole-2-thiomethyl]-1,3,4-thiadiazole (5). Furthermore, refluxing of 2,5-dimercapto-1,3,4-thiadizole (4) with chloroacetic acid yield 2,5-(dithioacetic acid)-1,3,4-thidiazole (6). Reaction of (6) with thiosemicarbazide in phosphoruse oxychloride gave 2,5-di-[5-amino-1,3,4-thiadiazole-2-thiomethyl]-1,3,4-thiadiazole (7). The newly synthesized compounds were characterized by CHNS elemental analysis, IR and NMR spectral data. The newly synthesized compounds werescreened for their in vitro antibacterial activity. The prepared compounds manifested promising biological activity.

Synthesis of New 1,2,4‐ and 1,3,4‐Oxadiazole …

N2 - In the present study, a new 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives were synthesized. Benzol hydrazine (2) was prepared by the hydrazinolysis of methyl benzoate (1) with hydrazine hydrate in abs. ethanol. Condensation of (2) with chloroacetic acid in phosphoruse oxychloride results in the formation of 2-phenyl-5-chloromethyl-1,3,4-oxadiazole (3), which on reaction with 2,5-dimercapto-1,3,4-thiadiazole in pyridine affords 2,5-di-[5-phenyl-1,3,4-oxadiazole-2-thiomethyl]-1,3,4-thiadiazole (5). Furthermore, refluxing of 2,5-dimercapto-1,3,4-thiadizole (4) with chloroacetic acid yield 2,5-(dithioacetic acid)-1,3,4-thidiazole (6). Reaction of (6) with thiosemicarbazide in phosphoruse oxychloride gave 2,5-di-[5-amino-1,3,4-thiadiazole-2-thiomethyl]-1,3,4-thiadiazole (7). The newly synthesized compounds were characterized by CHNS elemental analysis, IR and NMR spectral data. The newly synthesized compounds werescreened for their in vitro antibacterial activity. The prepared compounds manifested promising biological activity.

How to synthesize 1,3-oxadiazole? - ResearchGate

In the present study, a new 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives were synthesized. Benzol hydrazine (2) was prepared by the hydrazinolysis of methyl benzoate (1) with hydrazine hydrate in abs. ethanol. Condensation of (2) with chloroacetic acid in phosphoruse oxychloride results in the formation of 2-phenyl-5-chloromethyl-1,3,4-oxadiazole (3), which on reaction with 2,5-dimercapto-1,3,4-thiadiazole in pyridine affords 2,5-di-[5-phenyl-1,3,4-oxadiazole-2-thiomethyl]-1,3,4-thiadiazole (5). Furthermore, refluxing of 2,5-dimercapto-1,3,4-thiadizole (4) with chloroacetic acid yield 2,5-(dithioacetic acid)-1,3,4-thidiazole (6). Reaction of (6) with thiosemicarbazide in phosphoruse oxychloride gave 2,5-di-[5-amino-1,3,4-thiadiazole-2-thiomethyl]-1,3,4-thiadiazole (7). The newly synthesized compounds were characterized by CHNS elemental analysis, IR and NMR spectral data. The newly synthesized compounds werescreened for their in vitro antibacterial activity. The prepared compounds manifested promising biological activity.

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