scholarly journals Synthesis and In Vitro Antioxidant Evaluation of Some Novel 4, 5-Dihydro-1H, 2, 4-triazol-5-one Derivatives

2010 ◽  
Vol 7 (1) ◽  
pp. 123-136 ◽  
Author(s):  
O. Gursoy Kol ◽  
H. Yuksek

In this study, thirteen novel 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were synthesized and characterized by elemental analyses and IR,1H NMR,13C NMR and UV spectral data. The synthesized compounds were analyzed for theirin vitropotential antioxidant activities in three different methods. Those antioxidant activities were compared to standard antioxidants such as BHA, BHT andα-tocopherol. The data reveal that the compounds demonstrate a marked capacity for iron binding, especially5aand7cIn addition to this, the compounds4were titrated potentiometrically with TBAH in non-aqueous solvents because of the weak acidic properties of 4,5-dihydro-1H-1,2,4-triazol-5-one ring N-H group.

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
H. Yuksek ◽  
O. Akyildirim ◽  
O. Gursoy Kol

Nine new 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were synthesized and characterized by elemental analyses and IR,1H-NMR,13C-NMR and UV spectral data. The synthesized compounds were analyzed for theirin vitropotential antioxidant activities in three different methods. Those antioxidant activities were compared to standard antioxidants such as BHA, BHT andα-tocopherol. Compounds4e,5aand5dshowed best activity for iron binding. In addition, the compounds4were titrated potentiometrically with tetrabutylammonium hydroxide (TBAH) in four non-aqueous solvents (isopropyl alcohol,tert-butyl alcohol, acetone andN,N-dimethyl formamide). Thus, the half-neutralization potential values and the correspondingpKavalues were determined in all cases.


2009 ◽  
Vol 2009 (4) ◽  
pp. 261-264 ◽  
Author(s):  
Xiaowei Yan ◽  
Maolin Hu ◽  
Qian Miao ◽  
Shun Wang ◽  
Kejian Zhao

A new series of peptide 5-fluorouracil derivatives was designed and synthesised in order to test in vitro anticancer activities. The results indicated that peptide 5-fluorouracil derivatives possessed anticancer activities against human HL-60 and Bel-7402 cell lines. The structures of the compounds were determined by means of 1H NMR, 13C NMR, IR, mass spectra and elemental analyses.


2018 ◽  
Vol 22 (01n03) ◽  
pp. 233-242 ◽  
Author(s):  
Nazlı Söylemez ◽  
Ebru Yabaş ◽  
Serap Şahin Bölükbaşı ◽  
Mustafa Sülü

4-[(4′-(Tert-butyl)phenoxy)phenoxy]phthalonitrile 1 has been prepared by the reaction of 4-(4-nitrophenoxy)phthalonitrile with 4-tertiarylbutylphenole. 4-((4′-tert-butyl)phenoxy)phenoxy tetrasubstituted metal-free 2, zinc(II) 3 and cobalt(II) 4 phthalocyanines have been prepared by tetramerization of compound 1. The synthesized phthalocyanines showed high solubility in common organic solvents such as CHCl[Formula: see text]. All compounds were characterized by elemental analysis and [Formula: see text]H-NMR, [Formula: see text]C-NMR, UV-vis, IR spectra. Aggregation behaviors of these compounds have been investigated in different solvents (CHCl[Formula: see text], THF, DMF and DMSO) and different concentrations in CHCl[Formula: see text]. The in vitro antioxidant activities of phthalocyanine compounds 2, 3 and 4 were evaluated in a series of assays involving DPPH radicals, hydroxyl radicals, superoxide radicals, singlet oxygen and hydrogen peroxide. Antioxidant activity of compound 2was found to be higher than that of compounds 3 and 4.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Sankari Kanakaraju ◽  
P. Sagar Vijay Kumar ◽  
Bethanamudi Prasanna ◽  
G. V. P. Chandramouli

A series of novel pyranochromene-containing tetrazoles fused with pyrimidinethiones, pyrimidines, and diazepines 3a–f, 4a–f, and 5a–f were synthesized by condensation of the corresponding tetrazoles 2a–f with carbon disulfide, benzaldehyde, and 4-methoxy phenacyl bromide, respectively. The compound 2a–f was obtained by reaction of pyrano[3,2-c]chromenes 1a–f with sodium azide. The structures of the newly synthesized compounds 2a–f to 5a–f were established on the basis of their elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral data. All of the title compounds were subjected to in vitro antibacterial testing against four pathogenic strains and antifungal screening against two fungi. Preliminary results indicate that some of them exhibited promising activities and that they deserve more consideration as potential antimicrobials.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (10) ◽  
pp. 17-22
Author(s):  
Chaithra R Shetty ◽  
Ishwar K Bhat ◽  
Abhishek Kumar ◽  
Vijay Kumar Merugumolu ◽  
Revanasidappa BC ◽  
...  

Antioxidants exert their action chiefly in controlling and preventing the free-radicals and their reactions and thus it has a vital role as health protecting factor. There are many scientific data proposing that antioxidants lower the threats of some chronic diseases including cancer and heart disease. In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone, has been taken for the study and different novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcohol media. The resulting Schiff bases were made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds was done by IR, 1 H NMR and Mass spectroscopy. The same reaction was performed in the microwave assisted reaction condition and compared with conventional synthesis. In vitro antioxidant activities of compounds were performed by three different methods, out of which Compound TZ4 emerged as a promising molecule.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
N. D. Jayanna ◽  
H. M. Vagdevi ◽  
J. C. Dharshan ◽  
T. R. Prashith Kekuda

Some novel 1-(5,7-dichloro-1,3-benzoxazol-2-yl)-1H-pyrazolo[3,4-b]quinoline derivatives8(a–f) were synthesized by reacting 5,7-dichloro-2-hydrazino-1,3-benzoxazole4and substituted-2-chloro-3-quinoline carbaldehydes usingp-toluenesulfonic acid (PTSA) as a catalyst for the cyclisation. The target molecules have been characterized by IR,1H NMR,13C NMR, and mass spectral studies. The synthesized compounds were screened for biological activities, and some of the compounds have exhibited encouraging antibacterial and antioxidant activities. The compounds8aand8eshowed potent antibacterial activity, whereas the compounds8eand8fact as antioxidants.


2008 ◽  
Vol 63 (5) ◽  
pp. 548-554 ◽  
Author(s):  
Olcay Bekircan ◽  
Tevfik Özen ◽  
Nurhan Gümrükcüoğlu ◽  
Hakan Bektaş

A series of new 3-(4-chlorophenyl)-5-(pyridin-4-yl)-4-(arylmethyleneamino)-4H-1,2,4-triazole derivatives 3 were prepared in good yields by treatment of 4-amino-3-(4-chlorophenyl)-5-(pyridine- 4-yl)-4H-1,2,4-triazole (2) with selected aldehydes. Compounds 3 were reduced with NaBH4 to afford the corresponding 3-(4-chlorophenyl)-5-(pyridin-4-yl)-4-(arylmethylamino)-4H-1,2,4-triazole derivatives 4. Eighteen new compounds were synthesized and characterized by elemental analyses, IR, 1H NMR and 13C NMR spectral data. The compounds were screened for their antioxidant and antiradical activities.


1983 ◽  
Vol 48 (12) ◽  
pp. 3426-3432 ◽  
Author(s):  
Dušan Koščík ◽  
Pavol Kristian ◽  
Ondrej Forgáč

New synthesis of pyrido[3,4-e]-1,3-thiazines consisting in reaction of 2,6-dimethyl-4-chloronicotinoyl isothiocyanate with primary or secondary amines, or with benzaldehyde phenylhydrazone, is described. High reactivity of the chlorine atom does not allow isolation of the corresponding thioureas, arising as intermediates, except in the case of the benzylamino derivative. Structure of the products was unequivocally confirmed by their spectral data (IR, UV, 1H NMR, 13C NMR and mass spectra). The synthesized derivatives do not undergo the Dimroth rearrangement.


1998 ◽  
Vol 63 (3) ◽  
pp. 363-370 ◽  
Author(s):  
Violetta Patroniak-Krzyminiewska ◽  
Wanda Radecka-Paryzek

The template reactions of 2,6-diacetylpyridine with 3,6-dioxaoctane-1,8-diamine in the presence of dysprosium(III), thulium(III) and lutetium(III) chlorides and erbium(III) perchlorate produce the complexes of 15-membered macrocyclic ligand with an N3O2 set of donor atoms as a result of the [1+1] Schiff base cyclocondensation. In contrast, analogous reactions involving the lighter lanthanide ions (lanthanum(III), samarium(III) and europium(III)) yield the acyclic complexes with terminal acetylpyridyl groupings as products of the partial [2+1] condensation. The complexes were characterized by spectral data (IR, UV-VIS, 1H NMR, MS), and thermogravimetric and elemental analyses.


1993 ◽  
Vol 58 (1) ◽  
pp. 173-190 ◽  
Author(s):  
Eva Klinotová ◽  
Jiří Klinot ◽  
Václav Křeček ◽  
Miloš Buděšínský ◽  
Bohumil Máca

Reaction of 3β-acetoxy-21,22-dioxo-18α,19βH-ursan-28,20β-olide (IIIa) and 20β,28-epoxy-21,22-dioxo-19α,19βH-ursan-3β-yl acetate (IIIb) with diazomethane afforded derivatives XII-XIV with spiroepoxide group in position 21 or 22, which were further converted into hydroxy derivatives XV and XVII. Ethylene ketals VIII-X were also prepared. In connection with the determination of position and configuration of the functional groups at C(21) and C(22), the 1H and 13C NMR spectral data of the prepared compounds are discussed. Complete analysis of two four-spin systems in the 1H NMR spectrum of bisethylenedioxy derivative Xb led to the proton-proton coupling constants from which the structure with two 1,4-dioxane rings condensed with ring E, and their conformation, was derived.


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