scholarly journals Synthesis, Characterisation and Biological Screening of s-Triazine Based Chalcones and its Derivatization into Phenyl Pyrazolines, Isoxazoles

Author(s):  
Anjani Solankee ◽  
Riki Tailor

Heterocyclic derivatives such as phenyl pyrazolines and isoxaxoles were prepared from s - triazine based chalcones. Chalcones (A1 - A5) are synthesised by the reaction of compound (V) with various aromatic aldehydes. Moreover, further reaction of chalcones with phenyl hydrazine hydrochloride and hydroxylamine hydrochloride in the presence of alkali gives phenyl pyrazolines (A6 - A10) and isoxazoles (A11 - A15) derivatives respectively. The structures of the newly synthesised compounds were confiremed by spectroscopic (IR, 1H NMR, 13C NMR) and elemental analysis. All the newly synthesised compounds have been screened for their antimicrobial activity against selected Gram - positive (S. aureus and S. pyogenus), Gram - negative (E. coli and P. aeruginosa) bacterial and fungal strains (C. albicans, A. niger and A. clavatus).

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.


2008 ◽  
Vol 73 (7) ◽  
pp. 683-690 ◽  
Author(s):  
Dipti Dodiya ◽  
Amit Trivedi ◽  
Samir Jarsania ◽  
Shailesh Vaghasia ◽  
Viresh Shah

The synthesis of substituted pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidin-8-ones (IIIa-j) from 5-amino-3-methyl-1H-thieno[3,2-c]pyrazole-6-carbonitrile (II) is described. The key compound II was synthesized from (5-methyl- -2,4-dihydro-3H-pyrazol-3-ylidene)malononitrile I via the Gewald reaction. The synthesis of the title compounds IIIa-j was accomplished by condensation of II with different aromatic aldehydes. The newly synthesized heterocyles were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectroscopic investigation. All the newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains. .


2005 ◽  
Vol 2 (2) ◽  
pp. 109-112
Author(s):  
A. K. Parekh ◽  
K. K. Desai

Some new chalcones have been prepared by Claisen-schmidt condensation of ketone and different aromatic aldehydes. These chalcones on condensation with urea in presence of acid gave Pyrimidine-2-ones. The synthesized compounds have been characterized by elemental analysis, IR and1H NMR spectral data. They have been screened for their antibacterial activity against Gram positive bacteria B. subtillis & S. aureus and Gram negative bacteria E. coli & S. typhi.


2020 ◽  
Vol 32 (4) ◽  
pp. 789-794
Author(s):  
Chintan P. Somaiya ◽  
Dinesh S. Patel ◽  
Darshan H. Jani

In this work novel pyrazolone based semicarbazone derivatives and their spectroscopic and biological activities were investigated. Pyrazolone based semicarbazone ligands and their Fe(III) and Mn(III) heterochelates were synthesized. The structure of semicarbazone ligands were confirmed by 1H NMR, IR, elemental analysis and their heterochelates were confirmed by thermal studies (TGA/DTG & DSC) and FAB mass spectroscopy. All the ligands and heterochelates were screened for antimicrobial study against Gram positive (Bacillus megaterium, Bacillus subtilis) and Gram negative (E. coli, Klebsiella) microorganisms. The results confirmed that semicarbazone based heterochelates have a great potential and significant for further investigation.


2019 ◽  
Vol 24 (4) ◽  
Author(s):  
Nabeel Abed Abdul‐Reda ◽  
Miad Hassan jebur

Some new derivatives ofsuberic chloride synthesized by reactionssuberoyl chloride with 4-amino acetophenoneto prepare N1,N8-bis(4-acetylcyclohex-2-en-1-yl)octanediamide,then react with 4-nitrobenzaldehydein the presence of sodium hydroxide,the product reacted with (urea,thiourea, phenyl hydrazine, 2-amino aniline,2-aminophenol, 2,4-dinitrophenyl hydrazine and 2-amino benzothiol) to prepare many hetrocyclicderivatives. This reaction was checked by thin‐layer chromatography (TLC) method. All new compounds were characterized by melting points, elemental analysis, FT‐IR,1H&13C-NMR. The antibacterial action of these derivatives was determined.


Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.


2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.


2018 ◽  
Vol 69 (4) ◽  
pp. 815-822 ◽  
Author(s):  
Lucia Pintilie ◽  
Amalia Stefaniu ◽  
Alina Ioana Nicu ◽  
Maria Maganu ◽  
Miron Teodor Caproiu

A new series of fluoroquinolone compounds have been obtained by Gould-Jacobs method. The compounds have been characterized by physic-chemical methods (elemental analysis, FTIR, NMR, UV-Vis) and by antimicrobial activity against Gram-positive and Gram-negative microorganisms. For the synthesized compounds have been performed calculations of characteristics and molecular properties, using Spartan�14 Software from Wavefunction, Inc. Irvine, CA. and molecular docking studies using CLC Drug Discovery Workbench 2.4 software, to identify and visualize the most likely interaction ligand (fluoroquinolone) with the receptor protein.


2012 ◽  
Vol 9 (4) ◽  
pp. 1897-1905 ◽  
Author(s):  
A. Solankee ◽  
K. Patel ◽  
R. Patel

Chalcones(6a-f)have been prepared by the condensation of ketone(5)and different aromatic and heterocyclic aldehydes. These chalcones(6a-f)on treatment with guanidine hydrochloride and phenyl hydrazine hydrochloride in presence of alkali give aminopyrimidines(7a-f)and phenylpyrazolines(8a-f)respectively. All the newly synthesized compounds have been characterized on the basis of IR,1HNMR spectral data as well as physical data. Antibacterial activity (minimum inhibitory concentration MIC) against Gram-positiveS. aureusMTCC 96 andS. pyogeneusMTCC 442 and Gram-negativeP. aeruginosaMTCC 1688 andE. coliMTCC 443 bacteria, as well as antifungal acivities (MIC) againstC. albicansMTCC 227,A. nigerMTCC 282 andA. clavatusMTCC 1323 were determined by broth dilution method.


Author(s):  
Amita Shobha Rao ◽  
Shobha Kl ◽  
Prathibha Md’almeida ◽  
Kiranmai S Rai

  Objective: Infections caused by Gram-negative bacteria are important causes of morbidity and mortality. Extracts of plants and herbs such as Clitorea ternatea are used as diuretic. This work attempts to find out antimicrobial activity of aqueous and alcoholic extract of C. ternatea roots against Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), clinical strains of Klebsiella pneumoniae, and Candida albicans.Methods: The agar well-diffusion method was done using Mueller Hinton agar and Sabouraud’s dextrose agar. The microorganism grown in peptone water was inoculated into culture medium. 4 mm diameter well punched into the agar was filled with 20 μl of aqueous and alcoholic root extracts C. ternatea extracts in various concentrations (100-25 μg/ml). The plates were incubated and antimicrobial activity was evaluated.Results: Aqueous root extract of C. ternatea with the concentration of 100 μg/ml showed zone of inhibition against E. coli (ATCC 25922) 18 mm, P. aeruginosa (ATCC 27853) 14 mm, multidrug resistant strain of K. pneumoniae 15 mm. Alcoholic extract of C. ternatea with the concentration of 100 μg/ml showed zone of inhibition of 35 mm against E. coli (ATCC 25922), P. aeruginosa (ATCC 27853) 22 mm, and multidrug resistant strain of K. pneumoniae 28 mm. C. albicanswas resistant to both extract of C. ternatea root. Conclusions: Alcoholic extract of C. ternatea is a better antibacterial agent against multidrug resistant Klebsiella species and other Gram-negative pathogens. Further, studies are required to identify active substances from the alcoholic extracts of C. ternatea for treating infections.


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