scholarly journals The Synthesis, Characterization and Evaluation of Anti-microbial activity of some novel 1,2,4- trizaoles

Author(s):  
Alex Martin

Some novel 4-(aryliidineamino)-5-(1-(4-isobutylphenyl) ethyl)-4-yl-4H-1,2,4-triazole-3-thiols were prepared from the  reaction of carbon-di-sulphide and hydrazine hydrate in water to produce thiocarbohydrazides. The thiocarbohydrazides is then refluxed with ibuprofen for 2 hour, followed by cooling to room temperature and washing with sodium bicarbonate solution to produce  5-(1-(4-isobutylphenyl) ethyl)-4H-1,2,4- triazole-3-thiole. It is then refluxed with different aldehydes in the presence of ethanol and HCl to produce the title compounds. The synthesized compounds are recrystallized from ethanol and are analyzed for their physical and spectral data. They are screened for their anti-microbial activity and it was found that the title compounds are found to have moderate to good antimicrobial activity.

2011 ◽  
Vol 8 (2) ◽  
pp. 635-642 ◽  
Author(s):  
D. C. P. Singh ◽  
S. R. Hashim ◽  
R. G. Singhal

2-Chloro-3-methylquinoxaline was selected as nucleus around which the molecular manipulations were carried out to get new compounds expected to possess better anti microbial activity. Various quinoxaline derivatives have been synthesized by replacing the chlorine at C-2 with a thioether linkage, which in turn attached to 2-(N-(substituted phenyl)acetamides. The synthesized compounds (5) were tested for their antimicrobial activity. Compounds 5b, 5c, 5d and 5i were found most active (comparable to the standard antibacterial Ciprofloxacin) amongst them. The structure of the compounds was confirmed on the basis of their spectral data.


2018 ◽  
Vol 15 (1) ◽  
pp. 126-136 ◽  
Author(s):  
Ghada S. Masaret ◽  
Thoraya A. Farghaly

Aim and Objective: Enaminones belay to be extremely stable compounds and constitute a versatile group of salutary precursors for the synthesis of enormous classes of organic compounds. So, in this context, we synthesized a new enaminone, namely, (E)-3-(dimethylamino)-1-(8-phenyl-8H-[1,2,4]triazolo[4,3- a]perimidin-10-yl)prop-2-en-1-one (enaminone 2). Materials and Methods: The reaction of enaminone 2 with different types of hydrazonoyl chlorides or hydrazine hydrate afforded new substituted pyrazoles. Also, the reaction of enaminone with 6-amino-2- thioxopyrimidin-4-one in acetic acid under reflux produced 2-thioxopyridopyrimidinone derivative. The latter thione derivative reacts with hydrazonoyl chlorides to give pyridotriazolopyrimidines. 5-(8-Phenyl-8H- [1,2,4]triazolo[4,3-a]perimidin-10-yl)isoxazole was produced from the reaction of enaminone 2 with hydroxylamine. Results & Conclusion: The structure of all the novel perimidine derivatives was confirmed on the basis of spectral data and elemental analyses. The enaminone and the newly synthesized compounds were tested for their antimicrobial activity, and the results obtained revealed that some derivatives are more potent than the reference drugs used.


2019 ◽  
Vol 35 (2) ◽  
pp. 822-828
Author(s):  
Cong Tien Nguyen ◽  
Dao Thi Hong Dinh ◽  
Thin Van Nguyen ◽  
Giang Duc Le ◽  
Hien Cao Nguyen

4-Chlorobenzylidene-2-methyl-(4H)-oxazol-5-one, which were prepared from 4-chlorobenzaldehyde and acetylglycine in reaction with hydrazine hydrate in ethanol gave 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one. However, treatment of 4-chlorobenzylidene-2-methyl-(4H)-oxazol-5-one with hydrazine hydrate in pyridine yielded 3-(4-chlorophenyl)propanohydrazide. Reaction of 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one with aromatic aldehydes gave eight corresponding Schiff’s bases namely 1-arylideneamino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-ones. The structure of the 3-(4-chlorophenyl)propanohydrazide and the imidazoline-5-one compounds was confirmed by IR, 1H-NMR and MS spectral data. The Schiff’s bases were tested for antimicrobial activities against several strains of Gram-positive, Gram-negative bacteria, molds and yeasts.


1963 ◽  
Vol 22 (2) ◽  
pp. 335-340 ◽  
Author(s):  
J. W. Lassiter ◽  
M. K. Hamdy ◽  
Prasob Buranamanas

2019 ◽  
Vol 31 (9) ◽  
pp. 1895-1898
Author(s):  
Relangi Siva Subrahmanyam ◽  
Venkateswara Rao Anna

We report here an easy, efficient and green synthetic protocol for the (E)-1-aryl-3-(2-morpholinoquinolin-3-yl)prop-2-en-1-ones by the Claisen-Schmidt condensation of 2-morpholinoquinoline-3-carbaldehyde and different substituted acetophenones by using 1-butyl-3-methylimidazolium tetrafluoroborate (Bmim)BF4. The compounds were characterized by using 1H NMR, 13C NMR and mass spectral data and screened there in vitro antimicrobial activity against different bacterial and fungal organisms.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Liliana G. Fidalgo ◽  
Mário M. Q. Simões ◽  
Susana Casal ◽  
José A. Lopes-da-Silva ◽  
Ivonne Delgadillo ◽  
...  

AbstractHyperbaric storage at room temperature (HS/RT: 75 MPa/25 °C) of vacuum-packaged fresh Atlantic salmon (Salmo salar) loins was studied for 30 days and compared to atmospheric pressure at refrigerated temperatures (AP/5 °C, 30 days) and RT (AP/25 °C, 5 days). Most of the fatty acids were not affected by storage conditions, with only a slight decrease of docosahexaenoic acid (DHA) content (n-3 polyunsaturated fatty acid) for AP samples, reflected in the lower polyene index values obtained and higher oxidation extent. For HS, a lower lipid oxidation extension and a slower increase of myofibrillar fragmentation index values were observed, when compared to AP samples. The volatile profile was similar for the HS and fresh samples, with the HS samples retaining fresh-like alcohols and aldehydes components, which disappeared in AP samples, mainly in AP/25 °C samples. The volatile profile for AP samples (5 and 25 °C) revealed mostly spoilage-like compounds due to microbial activity. Drip loss increased progressively during the 30 days of storage under HS, while a slight decrease of water holding capacity after 5 days was observed, increasing further after 30 days. Regarding textural properties, only resilience was affected by HS, decreasing after 30 days. So, HS/RT could represent an interesting extended preservation methodology of fresh salmon loins, since allows retaining important physicochemical properties for at least 15 days, while refrigeration after 5 days showed already volatile spoilage-like compounds due to microbial activity. Furthermore, this methodology allows additional considerable energy savings when compared to refrigeration.


2021 ◽  
Vol 26 (2) ◽  
pp. 137-143
Author(s):  
S. N. Gromova ◽  
N. A. Guzhavina ◽  
E. A. Falaleeva ◽  
E. P. Kolevatykh ◽  
А. V. Elikov ◽  
...  

Relevance. A wide variety of oral care products is available nowadays. Sometimes aggressive advertising rather than doctor’s advice determines our patients’ choice. In our research, we provide evidence of the clinical use of toothpaste containing fluoride and sodium bicarbonate.Materials and methods. During four weeks, we followed up a group of students who used the toothpaste containing 1400 ppm fluoride and 67% aqueous sodium bicarbonate solution. The clinical, biochemical and microbiological tests and saliva crystallization score assessed the characteristics stated by the manufacturer.Results. The statistically significant correlation between all studied criteria is evidence of the effectiveness of the toothpaste. In addition to the significant remineralization and antiplaque effect, biochemical and microbiological tests confirmed the anti-inflammatory effect of the toothpaste. An immediate cleaning effect was observed after the first brushing as well as in long-term use.Conclusion. Improvement of oral hygiene indices and reduction of periodontal inflammation confirmed the successful result of the comprehensive treatment of chronic gingivitis.


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.


2009 ◽  
Vol 1 (2) ◽  
pp. 317-325 ◽  
Author(s):  
M. I. Hossain ◽  
M. M. H. Bhuiyan

Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6  dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitrile 1 with formic acid, affording 5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one 2, which is chlorinated with thionyl chloride and then hydrazinated with hydrazine hydrate. Finally hydrazino compound 4 is reacted with formic acid, acetic anhydrate, benzaldehyde, p-hydroxybenzaldehyde, p-toluayldehyde, p-nitrobenzaldehyde and p-chlorobenzaldehyde to give thienotriazolopyrimidines 5-6 and thienopyrimidines 7-11 respectively. All the compounds have been screened for their antimicrobial activity. Keywords: Fused pyrimidines; Hydrazino compound; Thienotriazolopyrmidines; Thienopyrimidines; Antimicrobial activity.© 2009 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.DOI: 10.3329/jsr.v1i2.2299


Sign in / Sign up

Export Citation Format

Share Document