scholarly journals Utility Of 6-Azauracils In Synthesis of New Poly Heterocyclic Nitrogen Systems Bearing 1,2,4-Triazine Moiety as Antioxidant Probes.

Author(s):  
Hafsa Sayed ◽  
Dina Bakhotma

Synthesis of new poly heterocyclic nitrogen systems containing 1,2,4-triazine moiety such as pyrazolines, pyrazolones, phthalazinone and 1,2,4-triazinone (9-17) have been deduced from hydrazinolysis of 3,5-dichloro-6,1-dihydro-1,2,4-triazine (2) which produced from the interaction between 6-azauracil (1) with POCl3/PCl5. Heterocyclization of 3,5-dihydrazino-1,2,4-triazine (7) by reaction nitrogen / oxygen / halogen bifunctional reagents in different mediums and conditions yielded the targets 9-17 respectively. Former structure of the products has been established from their elemental analysis and spectral data (UV, IR, 1H/13C NMR and Mass). All the new targets obtained evaluated as antioxidant probes in compare with ascorbic acid in 1,1-diphenyl-2-picrylhydrazyl (DPPH) as a standard, were the compounds 11>10>8>12>13 are more active probes.

2017 ◽  
Vol 68 (10) ◽  
pp. 2436-2439
Author(s):  
Stefania Felicia Barbuceanu ◽  
Laura Ileana Socea ◽  
Constantin Draghici ◽  
Elena Mihaela Pahontu ◽  
Theodora Venera Apostol ◽  
...  

In the work we presented the behavior of 5-(4-(4-X-phenylsulfonyl)phenyl)-4-(n-propyl)-2H-1,2,4-triazole-3(4H)-thiones (X= Cl or Br) with some alkylation agents. Thus, new S-alkylated 1,2,4-triazole derivatives were synthesized by reaction of the corresponding 1,2,4-triazole-3-thione derivatives with different �-halogenated compounds (ethyl bromide, ethyl chloroacetate or phenacyl bromide), in basic medium. The structures of synthesized compounds were elucidated by spectral data (1H-NMR, 13C-NMR, mass spectrometry) and elemental analysis.


2016 ◽  
Vol 4 (1) ◽  
pp. 10
Author(s):  
Amer A. Taqa

Some new metal(II) dichloride complexes with the ligands substituted nitrones of the general formula [ML2Cl2], where M= Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), L=OCH=CHCH=C-CH=N(O)C6H4X (X=H,p-CH3,CH3O,CH3CO,F,Cl,and Br) have been prepared and characterized by elemental analysis, IR,1H,13C NMR and Vis/Uv spectroscopy. The IR spectral data showed that the nitrone ligands coordinated with the metal ion through the most active atom of the N-oxide to give square planner coordinate (Cu,Ni,) complexes and (Zn,Cd,Co) tetrahedral complexes. No correlation was observed between the N-O vibrations stretching high frequency ν (N-O) of the complexes and the Hammet (σ) constants.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem

Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.


2007 ◽  
Vol 72 (4) ◽  
pp. 321-329 ◽  
Author(s):  
Sohel Mostahar ◽  
Sayed Alam ◽  
Azizul Islam

Two new 2'-oxygenated flavones have been synthesized via chalcone precursors and the biocidal activity of these two flavones, along with the corresponding chalcones against microbes (bacteria and fungi) and brine shrimp nauplii were investigated. Both the flavones (compounds 6 and 7) and their corresponding chalcones (compounds 4 and 5) showed good activity against all the tested bacterial and fungal strains. The LC50 values of compounds 4-7 were found to be 2.31, 0.94, 1.39 and 0.58 ?gmL -1, respectively. The synthesized compounds were characterized using UV-Vis, IR, 1H-NMR and 13C-NMR spectral data, together with elemental analysis. .


2017 ◽  
Vol 68 (11) ◽  
pp. 2503-2508 ◽  
Author(s):  
Laura Ileana Socea ◽  
Stefania Felicia Barbuceanu ◽  
Bogdan Socea ◽  
Constantin Draghici ◽  
Theodora Venera Apostol ◽  
...  

Acylhydrazinecarbothioamides (2a,b) were synthesized by addition of 2-(5H-dibenzo[a,d][7]annulen-5-yl)acetohydrazide to different isothiocyanates. The new 1,2,4-triazol-3-thioles (3a,b) were synthesized by cyclization of new 2- acylhydrazinecarbothioamides (3a,b) in basic media. Alkylation of 1,2,4-triazole-3-thiols (3a-c) with ethyl bromide gave only S-substituted derivatives (4a-c). The structures of the synthesized compounds have been established on spectral data (IR, 1H-NMR and 13C-NMR spectroscopy) and elemental analysis. The cytotoxic effect of new compounds was evaluated using two alternative models on plant and invertebrate organisms.


2008 ◽  
Vol 59 (7) ◽  
Author(s):  
George Bratulescu

This paper describes synthesis of new imidazo[1,2-a] pyridine derivatives. The products structures were confirmed by elemental analysis, 1H-NMR, and 13C-NMR.


2019 ◽  
Vol 16 (1) ◽  
pp. 165-172 ◽  
Author(s):  
Mohammed S.T. Makki ◽  
Reda M. Abdel-Rahman ◽  
Abdulrahman Salim Alharbi

Aim and Objective: It is known that the Lamotrigine drug has anti-inflammatory activity. So it was the goal to prepare similar compounds containing fluorine atoms (fluorine-substituted 3,5-diamino-6-aryl- 1,2,4-triazines) as Lamotrigine drug analogs to evaluate them as an anti-inflammatory. Materials and Methods: The novel fluorine substituted 3,5-diamino-6-aryl-1,2,4-triazines as new Lamotrigine analogs were prepared via aminolysis and/ or ammonolysis of the corresponding 3-thioxo-6-aryl-1,2,4-triazin- 5-ones in ethanolic media. </P><P> Results: All the new targets were deduced upon their elemental analysis and spectral data as well as screened as anti-inflammatory agents, where we found that the fluorinated systems 15 and 9-11 exhibited high and more activity. Conclusion: Simple routes to synthesize some more novel fluorinated Lamotrigine analogs have been reported. The new targets exhibited high and moderate anti-inflammatory probes. Presence of both amino and CF3 groups caused high biological activities of these compounds were studied.


2008 ◽  
Vol 59 (4) ◽  
Author(s):  
Gabriela Laura Almajan ◽  
Stefania Felicia Barbuceanu ◽  
Ioana Saramet ◽  
Mihaela Dinu ◽  
Cristian Vasile Doicin ◽  
...  

5-[4-(4X-phenylsulfonyl)phenyl]-1,3,4-oxadiazole-2-thiols, X=H, Cl, Br, reacted with ethyl chloroacetate to give S-alkylated compounds. Aminomethylation of the thione form of oxadiazoles yielded N(3)-derivatives. All the products have been characterized by elemental analysis, IR, 1H-NMR and 13C-NMR. The plant-growth regulating effects of the title compounds were examined. From the biological activity results, we found that most compounds showed weak stimulatory activities at low concentrations.


2018 ◽  
Vol 17 (6) ◽  
pp. 448-457 ◽  
Author(s):  
Xia Huang ◽  
Tie Chen ◽  
Rong-Bi Han ◽  
Feng-Yu Piao

Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1). Conclusion: Possible structure-activity relationship was discussed.


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