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Search Results: 1 - 10 of 1232 matches for " Thiazole derivatives "
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A pyrazolyl-thiazole derivative causes antinociception in mice
Prokopp, C.R.;Rubin, M.A.;Sauzem, P.D.;de Souza, A.H.;Berlese, D.B.;Lourega, R.V.;Muniz, M.N.;Bonacorso, H.G.;Zanatta, N.;Martins, M.A.P.;Mello, C.F.;
Brazilian Journal of Medical and Biological Research , 2006, DOI: 10.1590/S0100-879X2006000600013
Abstract: the present study investigates the antinociceptive effect of the pyrazolyl-thiazole derivative 2-(5-trichloromethyl-5-hydroxy-3-phenyl-4,5-dihydro-1 h-pyrazol-1-yl)-4-(4-bromophenyl)-5-methylthiazole (b50) in mice. male albino swiss mice (30-40 g) were used in the acetic acid-induced abdominal writhes and tail-immersion tests. b50 caused dose-dependent antinociception (8, 23 and 80 μmol/kg, sc) in the acetic acid writhing assay (number of writhes: vehicle: 27.69 ± 6.15; b50 (8 μmol/kg): 16.92 ± 3.84; b50 (23 μmol/kg): 13.85 ± 3.84; b50 (80 μmol/kg): 9.54 ± 3.08; data are reported as means ± sem for 9 animals per group). on the other hand, b50 did not cause antinociception in the tail immersion assay. naloxone (2.75 μmol/kg, sc) prevented b50-induced antinociception (number of writhes: vehicle-saline: 31.11 ± 3.15; vehicle-naloxone: 27.41 ± 3.70; b50 (80 μmol/kg)-saline: 8.70 ± 3.33; b50 (80 μmol/kg)-naloxone: 31.84 ± 4.26; morphine-saline: 2.04 ± 3.52; morphine-naloxone: 21.11 ± 4.26; 8-9 animals per group). the removal of the methyl group of the thiazole ring of b50 or substitution of the bromo substituent with the methyl at position 4 of the phenyl group, which is attached to the thiazole ring of b50, resulted in loss of activity, suggesting that these substituents are important for antinociceptive activity. b50 had no effect on spontaneous locomotion or rotarod performance, indicating that the antinociceptive effect of b50 is not related to nonspecific motor effects. the antinociceptive profile of b50 seems to be closer to nonsteroidal anti-inflammatory drugs than to classic opioid agents, since it had no analgesic effect in a thermally motivated test.
Inhibition of glutamate dehydrogenase and insulin secretion by KHG26377 does not involve ADP-ribosylation by SIRT4 or deacetylation by SIRT3
Eun-A Kim1,#, Seung-Ju Yang2,#, Soo Young Choi3, Woo Je Lee4,* & Sung-Woo Cho1,*
BMB Reports , 2012,
Abstract: We investigated the mechanisms involved in KHG26377 regulationof glutamate dehydrogenase (GDH) activity, focusing onthe roles of SIRT4 and SIRT3. Intraperitoneal injection of micewith KHG26377 reduced GDH activity with concomitant repressionof glucose-induced insulin secretion. Consistent withtheir known functions, SIRT4 ribosylated GDH and reduced itsactivity, and SIRT3 deacetylated GDH, increasing its activity.However, KHG26377 did not affect SIRT4-mediated ADP-ribosylation/inhibition or SIRT3-mediated deacetylation/activationof GDH. KHG26377 had no effect on SIRT4 protein levels,and did not alter total GDH, acetylated GDH, or SIRT3 proteinlevels in pancreatic mitochondrial lysates. These results suggestthat the mechanism by which KHG26377 inhibits GDHactivity and insulin secretion does not involve ADP-ribosylationof GDH by SIRT4 or deacetylation of GDH by SIRT3.
A pyrazolyl-thiazole derivative causes antinociception in mice
Prokopp C.R.,Rubin M.A.,Sauzem P.D.,de Souza A.H.
Brazilian Journal of Medical and Biological Research , 2006,
Abstract: The present study investigates the antinociceptive effect of the pyrazolyl-thiazole derivative 2-(5-trichloromethyl-5-hydroxy-3-phenyl-4,5-dihydro-1 H-pyrazol-1-yl)-4-(4-bromophenyl)-5-methylthiazole (B50) in mice. Male albino Swiss mice (30-40 g) were used in the acetic acid-induced abdominal writhes and tail-immersion tests. B50 caused dose-dependent antinociception (8, 23 and 80 μmol/kg, sc) in the acetic acid writhing assay (number of writhes: vehicle: 27.69 ± 6.15; B50 (8 μmol/kg): 16.92 ± 3.84; B50 (23 μmol/kg): 13.85 ± 3.84; B50 (80 μmol/kg): 9.54 ± 3.08; data are reported as means ± SEM for 9 animals per group). On the other hand, B50 did not cause antinociception in the tail immersion assay. Naloxone (2.75 μmol/kg, sc) prevented B50-induced antinociception (number of writhes: vehicle-saline: 31.11 ± 3.15; vehicle-naloxone: 27.41 ± 3.70; B50 (80 μmol/kg)-saline: 8.70 ± 3.33; B50 (80 μmol/kg)-naloxone: 31.84 ± 4.26; morphine-saline: 2.04 ± 3.52; morphine-naloxone: 21.11 ± 4.26; 8-9 animals per group). The removal of the methyl group of the thiazole ring of B50 or substitution of the bromo substituent with the methyl at position 4 of the phenyl group, which is attached to the thiazole ring of B50, resulted in loss of activity, suggesting that these substituents are important for antinociceptive activity. B50 had no effect on spontaneous locomotion or rotarod performance, indicating that the antinociceptive effect of B50 is not related to nonspecific motor effects. The antinociceptive profile of B50 seems to be closer to nonsteroidal anti-inflammatory drugs than to classic opioid agents, since it had no analgesic effect in a thermally motivated test.
SYNTHESIS AND DOCKING STUDIES OF 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDE DERIVATIVES
K. Hemalatha*, Nandakishore Agarwal and G. Buchappa
International Journal of Pharmaceutical Sciences and Research , 2013,
Abstract: A novel N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-pipear azinyl]-2-methyl-4-pyrimidinyl] amino]-5-thiazolecarboxamide derivatives (6a-6d) and (8a-8b) were synthesized by coupling 2-[(6-chloro-2-methylpyrimidin-4ylamino]-N-(2-chloro-6-methylphenyl) thiazole-5-Carboxamide(3) with Piperazine derivatives(4,7) in butanol and DIPEA (Diisopropylethylamine) at 120oC for 4-5hrs. All the synthesized compounds were characterized physically and elucidated by Infrared spectroscopy, Mass spectroscopy, 1H-NMR spectroscopic techniques. All the synthesized compounds were subjected to Molecular docking studies by using 2GQG as its PDB ID. Among all the compounds, 6a, 6b, 6d, 8c and 8b exhibit anticancer activity.
Synthesis, Reactions and Antimicrobial Activities of 8-Ethoxycoumarin Derivatives
Hany M. Mohamed,Ashraf H. F. Abd El-Wahab,Kamal A. Ahmed,Ahmed M. El-Agrody,Ahmed H. Bedair,Fathy A. Eid,Mostafa M. Khafagy
Molecules , 2012, DOI: 10.3390/molecules17010971
Abstract: Condensation of 3-acetyl-8-ethoxycoumarin (3) with thiosemicarbazide gave ethylidenehydrazinecarbothioamide 5, which was transformed into the thiazolidin-4-one derivatives 6,7. Interaction of 3 with DMF/POCl3 gave b-chloroacroline derivative 8. Treatment of 3 with malononitrile gave benzo[c]chromone and 2-aminobenzonitrile derivatives 9 and 10, respectively with respect to the reaction conditions. Condensation of 3-(2-bromoacetyl)-8-ethoxycoumarin (4) with o-phenylenediamine gave 3-(quioxaline-2-yl)-8-ethoxycoumarin hydrobromide (11), while 4 reacted with 2-aminopyridine to give chromenopyridopyrimidine derivative 12. Condensation of 4 with potassium thio-cyanate/methanol gave an unexpected derivative, 2H-chromeno-3-carboxy(methyl-carbonimidic)thioanhydride 16, which upon treatment with (NH2)2·H2O gave 3-ethoxy-2-hydroxybenzaldehyde azine 19. Interaction of 4 with thiourea derivatives gave thiazole derivatives 20a–c. The structures of the newly synthesized compounds were confirmed by their spectra data. The newly synthesized compounds were also screened for their antimicrobial activity.
INHIBITION OF SPLEEN TYROSINE KINASE (SYK) IN SILICO BY THIAZOLE DERIVATIVES
S. J. Takate,S. S. Jadhav,Gaikar Rajendra Babasaheb,A. S. Burungale
International Research Journal of Pharmacy , 2013,
Abstract: Variously substituted thiazoles derivatives showed wide range of biological activity. The computational evaluation of the substituted thiazole containing derivatives as SYK inhibitor was performed. By using online servers applying different approaches the Tyrosine protein kinase (SYK) was identified as target for variously substituted thiazole containing derivatives. The molecular descriptor analysis was performed to identify drug likeness of the thiazole derivatives by Lipinski’s rule of five. Then docking analysis was performed by PyRx software using AutoDock vina 4. Derivatives showed comparatively significant binding energy value followed Lipinski’s rule. The study provides the base for further in vitro and in vivo study of substituted azoles containing compounds as SYK inhibitor and proposed drug to be used for allergic diseases.
Thiazole derivatives as corrosion inhibitors for C-steel in sulphuric acid solution
Abd El-Aziz Fouda,Ahmed Al-Sarawy,Emad El-Katori
European Journal of Chemistry , 2010, DOI: 10.5155/eurjchem.1.4.312-318.105
Abstract: 5-phenylazo-2-thioxo-thiazolidin-4-one and four of its derivatives have been investigated as corrosion inhibitors for C-steel in 1 M sulphuric acid solution using weight-loss and galvanostatic polarization techniques. The efficiency of the inhibitors increases with increase in inhibitor concentration but decreases with a rise in temperature. The conjoint effect of the thiazole derivatives and KBr, KSCN and KI has also been studied. The apparent activation energy (Ea*) and other thermodynamic parameters (ΔS*, ΔH* and ΔG*ads) for the corrosion process have also been calculated. The galvanostatic polarization data indicated that, the inhibitors were of mixed-type, but the cathode is more polarized than the anode. The slopes of the cathodic and anodic Tafel lines ( c and a) are approximately constant and independent of the inhibitor concentration. The adsorption of these compounds on C-steel surface has been found to obey the Temkin's adsorption isotherm. The mechanism of inhibition was discussed in the light of the chemical structure of the undertaken inhibitors.
EXPLORING POTENTIAL OF 4-THIAZOLIDINONE: A BRIEF REVIEW
MULAY ABHINIT,MANGESH GHODKE,NIKALJE ANNA PRATIMA
International Journal of Pharmacy and Pharmaceutical Sciences , 2009,
Abstract: Thiazolidinone, a saturated form of thiazole with carbonyl group on fourth carbon, has been considered as a magic moiety (wonder nucleus) which posses almost all types of biological activities. This diversity in the biological response profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. Present article is sincere attempt to review chemistry, synthesis, spectral studies and applications of 4-thiazolidinone.
Preparation of α-Bromoketones and Thiazoles from Ketones with NBS and Thioamides in Ionic Liquids  [PDF]
Yuhta Izumisawa, Hideo Togo
Green and Sustainable Chemistry (GSC) , 2011, DOI: 10.4236/gsc.2011.13010
Abstract: Ketones smoothly reacted with NBS in the presence of a catalytic amount of ptoluenesulfonic acid to give α-bromoketones in good yields in typical ionic liquids, such as [bmim]PF6 and [bmpy]Tf2N, and the ionic liquids could be repeatedly used for the same reaction after the extraction of the α-bromoketones. Then, the one-pot conversion of ketones into thiazoles by the treatment with NBS, and subsequently with thioamides could be also carried out in [bmim]PF6 and [bmpy]Tf2N, respectively Thus, [bmim]PF6 and [bmpy]Tf2N could be used as recyclable reaction media for the preparation α-bromoketones and thiazoles from ketones.
Thiazole and Oxazole Alkaloids: Isolation and Synthesis
Danilo Davyt,Gloria Serra
Marine Drugs , 2010, DOI: 10.3390/md8112755
Abstract: Thiazoles, oxazole and their corresponding reduced derivatives, thiazolines and oxazolines, are found in marine sources exhibiting significant biological activities. The isolation, synthetic, and biological studies of these natural products, covering literature from January 2007 to June 2010, are summarized.
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