scholarly journals Synthesis, Characterization and Biological Activity of (E)-9-Benzylidene-5-phenyl-5,6,7,8,9,10-hexahydro-[1,2,4]triazolo[3,4-ɑ]quinazoline

2020 ◽  
Vol 15 (3) ◽  
pp. 111-118

Abstract: Novel quinazoline derivatives were synthesized viathe reaction of unsaturated carbonyl compound subsidiaries with 3-aminotriazole. These compounds are convenient and important intermediates for the synthesis of a rangeof useful and novel heterocyclic compounds. The structures of these compounds were characterized using elemental analysis and IR, 1H NMR and mass spectroscopic methods.They were also tested with respect to their anti-bacterial activity against two types of bacteria,Staphylococcus aureusand Pseudomonas aeruginosa. Significant anti-bacterial activity was observed,and the results indicate the favorable effect of electron-releasing substituents on anti-bacterial activity

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.


2012 ◽  
Vol 554-556 ◽  
pp. 1849-1852
Author(s):  
Hui Zhang ◽  
Min Fan Wu ◽  
Yu Tian ◽  
Jian Tong ◽  
Li Hong Shang

More new phenoxypropylamines have been synthesized. All the products have been characterized by elemental analysis, 1H-NMR, 1C-NMR and MS. The biological activity effects of the title compounds were examined. From the biological activity reSuperscript textsults, we found that some of them showed significant gastric acid antisecretory activity.


Author(s):  
Pratiksha S. Rathod ◽  
Shilpa G. Chavan

Pyrazolines are important nitrogen containing 5-membered heterocyclic compounds. Various, pyrazoline derivatives have been found to possess considerable biological and pharmaceutical applications as activities, which stimulated the research activity in this field. The chlorinated 3,5-diary-l-2-pyrazolines has been synthesized by reaction of appropriately substituted chloro chalcones and mono-substituted hydrazine’s have been synthesized. These compounds were characterized using IR, 1H-NMR and Mass spectra and Elemental analysis. They possess some potent biological activities. Therefore, biological screening of novel compounds has been also done.


2020 ◽  
Vol 16 (4) ◽  
pp. 415-418
Author(s):  
Zi-Hui Yang ◽  
Gong-Zheng Yang ◽  
Yue-Yue Qi

Background: Triclopyr(Dow-503), whose commercial name was green grass, was an internal absorption and selective novel herbicide, developed by Dow agricultural sciences using the basic structure of 2,4-D. Triclopyr was suitable for preventing broadleaf weeds for removing shrubs, maintaining fireproof lines, raising pine trees and forest areas. Moreover, it could be used in paddy fields to prevent some broad-leaved weeds at the dose of 150-500g/hm. Methods: Two novel Triclopyr derivatives were synthesized based on the structure of commerical herbicide Triclopyr. Their structures were confirmed by 1H NMR melting point and elemental analysis. The preliminary bioassay were also evaluated. Results: The preliminary bioassay results showed that the title compounds had some herbicidal activities at the dosage of 150 g/hm2.The compound 1 and 2 show the 100% inhibition against three kinds of test weeds. Further test revealed that compound 2 showed the 100% inhibition against the Amaranthus. The safety test for crop revealed that the compound 2 was safe for paddy at the dosage of 150 g/hm2. Conclusion: The two compounds can be used as the leading compounds with certain optimized value.


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.


2021 ◽  
Vol 25 (11) ◽  
pp. 157-169
Author(s):  
Ch. Sunitha ◽  
G. Brahmeshwari

A novel series of 3-arylbenzylidene-1H-benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dione (4a-l) was synthesized in moderate to good yields. The structures of the newly synthesized compounds were confirmed by 1H NMR, 13C NMR mass spectrometry and elemental analysis. The synthesized compounds were evaluated for their anti-bacterial and anti-oxidant activities. Among all the derivatives tested, the compound 3-(3,5- dimethoxy benzylidene)-1H-benzo [4,5]imidazo[2,1- c][1,4]oxazine-1,4-(3H)-dione showed more potent activity and 3-(4-methoxybenzylidene)-1H benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dion exhibited good activity as compared to standard streptomycin. The anti-fungal activity reveals that the compound 3- (3,5-dimethoxy benzylidene)-1H-benzo[4,5]imidazo [2,1-c][1,4]oxazine-1,4-(3H)-dione showed more promising activity as compared to standard Itrazole. The remaining compounds showed moderate to poor activity. Similarly, the anti-oxidant activity results revealed that the compound 3-(3,5-dimethoxy benzylidene)-1H-benzo [4,5] imidazo[2,1-c][1,4] oxazine-1,4-(3H)-dione exhibited potent activity as compared to the other tested compounds.


2018 ◽  
Vol 68 (12) ◽  
pp. 2761-2764
Author(s):  
Laura Ileana Socea ◽  
Stefania Felicia Barbuceanu ◽  
Constantin Draghici ◽  
George Mihai Nitulescu ◽  
Gabriel Saramet ◽  
...  

In this paper we present the synthesis of the new heterocyclic compounds with 5H-dibenzo[a,d][7]annulene moiety obtained by cyclization of 2-acylhydrazinecarbothioamides (2a,b). The acylhydrazinecarbothioamides were obtained by treating 2-(5H-dibenzo[a,d][7]annulen-5-yl)acetohydrazide (1) with 2,5-difluorophenyl or 3-bromophenyl isothiocyanates. 2-Amino-1,3,4-oxadiazoles (3a,b) were synthesized by cyclization of 2- acylhydrazinecarbothioamides in the presence of mercury oxide. The new 1,2,4-triazole-3-thioles (4a,b) were synthesized by cyclization, in alkaline media, of the corresponding acylhydrazinecarbothioamide. The structures of the new compounds synthesized were investigated by 1H-NMR, 13C-NMR, IR and elemental analysis.


2006 ◽  
Vol 60 (3) ◽  
Author(s):  
J. Qu ◽  
G. Sun ◽  
L. Wang ◽  
L. Qu

AbstractA new 4-[1-(4-methylphenylsulfonyl)-1H-indol-3-yl]but-3-en-2-one thiosemicarbazone (HL) was synthesized derived from 4-[1-(4-methylphenylsulfonyl)-1H-indol-3-yl]but-3-en-2-one. Four transition metal(II) complexes of HL have been prepared. Elemental analysis, molar conductivity, IR, UV, 1H NMR spectra, and TG-DTA have been used to characterize these complexes. The complexes have the general formula ML2, where M = Zn, Cu, Co, and Ni. The ligand and its complexes have been studied for their possible biological activity including anti-inflammatory, antibacterial, and antitumour activity in vitro.


2020 ◽  
Vol 17 ◽  
Author(s):  
Taghreed A. Alsufyani ◽  
Hosam A. Saad ◽  
Asmaa A. A. Al-otaibi

: Novel polyheterocyclic nitrogen systems such as 2-amino-1H-pyrazolo[5',1':3,4][1,2,4]-triazino[5,6-b]indole-3-carbonitrile 2, which has been synthesized for the first time in the present work, is considered as starting material for the synthesis of more novel polyheterocyclic systems with five fused rings and sometime eight fused rings via heterocyclization with α,β-bifunctional reagents under different conditions. The formed structures of the products were established from their correct elemental analysis and spectral data. Some of the compounds were evaluated for their antimicrobial activity using the Agar Well Diffusion method. Compounds 2, 4, 5, 6, 8 were found to be biologically active (Supplementary information).


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (08) ◽  
pp. 14-20
Author(s):  
S. S Kerur ◽  
◽  
K. R Alagawadi ◽  
H. Zhu ◽  
F. V Manvi

In the present study, synthesis and antimicrobial activity of 2,5-disubstituted triazole derivatives 5a-f are described. The structures of the newly synthesized compounds were confirmed by FTIR, 1H NMR, mass and elemental analysis. All compounds were screened for antitubercular and antibacterial activity. The results revealed that most of the compounds showed high or moderate biological activity against tested microorganisms.


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