scholarly journals Synthesis and Antimicrobal Activities of some Novel Triazolo[1,5-a]Pyrimidine Derivatives

2014 ◽  
Vol 30 ◽  
pp. 127-134 ◽  
Author(s):  
Sagar P. Gami ◽  
Kalpesh V. Vilapara ◽  
Hasmukh R. Khunt ◽  
Jayesh S. Babariya ◽  
Yogesh T. Naliapara
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Sodium Methoxide ◽  
Pyrimidine Derivatives ◽  
Ketene Dithioacetals ◽  
Convenient Synthesis ◽  
Bacteria And Fungi ◽  
C Nmr

A convenient synthesis of substituted 1,2,4-triazolo[1,5-a]pyrimidine was carried out by the reaction of various ketene dithioacetals with 5-amino 1,2,4-triazole in methanol in presence of sodium methoxide. The newly synthesized compound were characterized by 1H NMR, 13C NMR, IR, MS, elemental analysis and screened for their antimicrobial activity against various strains of bacteria and fungi.

scholarly journals Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

2016 ◽  
Vol 65 ◽  
pp. 11-26
Author(s):  
Nilesh M. Thumar ◽  
Ankur A. Kaneria ◽  
Milan Vadodaria ◽  
Kartik Ladva
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Pyrimidine Derivatives ◽  
Gram Negative ◽  
H Nmr ◽  
Ketene Dithioacetals ◽  
Convenient Synthesis ◽  
Bacteria And Fungi

A convenient synthesis of substituted Pyrazolo[1,5-a]pyrimidine was carried out by the reaction of different ketene dithioacetals with different aromatic amine in isopropanol in the presence of potassium carbonate. The newly synthesized compound were characterized by1H NMR, IR, Mass and screened for their antimicrobial activity against various strains of bacteria and fungi. From the synthesized different NCEs, compounds 8a, 8d and 8e are broad spectrum drug which can inhibit the growth of gram positive, gram negative bacteria and fungi.

scholarly journals Synthesis and Antimicrobial Screening 6-Aryl-2-(Amino/Methoxy)-4-[(4′-Difluoro Methoxy) (3′-Hydroxy) Phenyl] Nicotinonitrile

2015 ◽  
Vol 50 ◽  
pp. 35-42 ◽  
Author(s):  
Vijay N. Bhadani ◽  
Piyush A. Patel ◽  
Heta D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Sodium Methoxide ◽  
Ammonium Acetate ◽  
Mass Spectral Data ◽  
Antimicrobial Screening ◽  
Mass Spectral ◽  
Efficient Route

A series of an easy and efficient route for the synthesis of some new 2-amino-3-cyanopyridine (4a-4i) and 2-methoxy-3-cyanopyridine (5a-5i) derivatives were synthesized through the reaction of various chalcone (3a-3i) with malononitrile in presence of ammonium acetate and sodium methoxide, respectively. The constitutions of the all synthesized compounds have been established by the IR, 1H-NMR, Mass spectral data and Elemental analysis. Furthermore, all the synthesized products were screened for their antimicrobial activity.

scholarly journals Synthesis and Antimicrobial Activity of 2-{4'-[(4"-Aryl)-3"-Cyano-2"-Methoxy-Pyridine-6"-yl]-Phenyl Amino}-6-[Bis(2"'-Chloroethyl) Amino]-4-Methoxy-1,3,5-Triazine

2015 ◽  
Vol 49 ◽  
pp. 143-148
Author(s):  
P.J. Kathiriya ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Sodium Methoxide ◽  
Mass Spectra ◽  
Biological Activities ◽  
H Nmr ◽  
Bacteria And Fungi

The titled compounds (5a-5k) have been synthesized by the condensation of 2-{4'-[(3"-aryl)-2"-Propene-1"-one]-Phenyl amino}-6-[Bis-2""-chloroethyl) amino]-4-methoxy-1,3,5-triazine with malono nitrile in the presence of sodium methoxide. The biological activities of these compounds have been determined against various Gram +ve, Gram –ve bacteria and fungi. The constitutions of the products are supported by IR, 1 H NMR, Mass spectra and elemental analysis.

scholarly journals Synthesis of New Furothiazolo Pyrimido Quinazolinones from Visnagenone or Khellinone and Antimicrobial Activity

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem
Keyword(s):  
Antimicrobial Activity ◽  
Growth Inhibition ◽  
Spectral Data ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Heterocyclic Compounds ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Bacteria And Fungi ◽  
New Compounds

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.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

scholarly journals Characterization and biological evaluation of some novel pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidin-8-ones synthesized via the Gewald reaction

2008 ◽  
Vol 73 (7) ◽  
pp. 683-690 ◽  
Author(s):  
Dipti Dodiya ◽  
Amit Trivedi ◽  
Samir Jarsania ◽  
Shailesh Vaghasia ◽  
Viresh Shah
Keyword(s):  
Antimicrobial Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Spectroscopic Investigation ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Gewald Reaction ◽  
Compound Ii

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. .

Synthesis of New Phenoxypropylamines and Evaluation of their Antiulcer Activity as H2 -Receptor Antagonist

2012 ◽  
Vol 554-556 ◽  
pp. 1849-1852
Author(s):  
Hui Zhang ◽  
Min Fan Wu ◽  
Yu Tian ◽  
Jian Tong ◽  
Li Hong Shang
Keyword(s):  
Biological Activity ◽  
Receptor Antagonist ◽  
Gastric Acid ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Antiulcer Activity ◽  
Antisecretory Activity ◽  
C Nmr

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.

Synthesis of Nitro-Substituted 4-Oxo-4H-pyrimido[2,1-b]benzothiazole-3-carboxylic Acids and Their Spectral Characteristics

1995 ◽  
Vol 60 (4) ◽  
pp. 583-593 ◽  
Author(s):  
Alexander Bartovič ◽  
Dušan Ilavský ◽  
Ondrej Šimo ◽  
Lubomír Zalibera ◽  
Anna Belicová ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acids ◽  
Elemental Analysis ◽  
Nmr Spectra ◽  
Spectral Characteristics ◽  
C Nmr

The Gould-Jacobs reaction of all position isomeric 2-aminonitrobenzothiazoles II with diethyl ethoxy- methylenemalonate has been studied. The structure of substitution (IV) and cyclization (VI) products and of the corresponding acids (VIII) was confirmed by elemental analysis, IR, UV, 1H and 13C NMR spectra. Analogous derivatives III, V and VII, derived from the unsubstituted 2-aminobenzothiazole I, were used as standards in interpretation of the spectra. The synthesized derivatives I - VIII were tested for antimicrobial activity.

scholarly journals Cytotoxic and antimicrobial activities of two new synthetic 2'-oxygenated flavones reported from andrographis viscosula

2007 ◽  
Vol 72 (4) ◽  
pp. 321-329 ◽  
Author(s):  
Sohel Mostahar ◽  
Sayed Alam ◽  
Azizul Islam
Keyword(s):  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Brine Shrimp ◽  
Antimicrobial Activities ◽  
Good Activity ◽  
Biocidal Activity ◽  
Fungal Strains ◽  
Bacteria And Fungi

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. .

scholarly journals SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF NOVEL PYRAZOLO[3,4-b]PYRIDINES AND THEIR SPIRO-HETEROCYCLIC DERIVATIVES

2014 ◽  
Vol 10 (7) ◽  
pp. 2901-2915 ◽  
Author(s):  
Shawkat A. Abdelmohsen ◽  
Talaat I El Emary
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Aldehydes ◽  
Antibacterial And Antifungal Activity ◽  
Pyrimidine Derivatives ◽  
Spiro Derivatives ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
New Compounds ◽  
Hydrazone Derivative

The present work describes the synthesis of a novel series of heterocyclic moieties derived from 5-acetylpyrazolo[3,4-b]pyridine (1). The formation of chalcones (2a-d) was utilized to synthesize pyrazoline, isoxazoline and pyrimidine derivatives (3-10). Thiosemicarbazone and semicarbazone (11, 17) were utilized to synthesize other new triazolethiones, thiadiazole and selenadiazole derivatives (11-19). Some new spiro derivatives (22-25) were synthesized by the reaction of chalcone (21) of 1 and isatine with hydrazines, hydroxyl amines and thiourea. Also, The reaction of 1 with cyanoacetyl hydrazine gave the hydrazide-hydrazone derivative 26, which was allowed to react with aromatic aldehydes and α-cyanocinnamonitrile to afford coumarine and substituted pyridine derivatives (28, 29). The structures of all the new compounds have been established on the basis of their analytical and spectral data. Twenty two of the synthesized compounds were also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi and most are found to possess promising antimicrobial activity when compared with Chloramphenicol and Clotrimazole

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