scholarly journals Synthesis and Antifungal Activity of Azetidinone and Thiazolidinones Derivatives of 2-Amino-6-(2-naphthalenyl)thiazolo[3,2-d]thiadiazole

2006 ◽  
Vol 3 (4) ◽  
pp. 267-273 ◽  
Author(s):  
K. H. Patel ◽  
A. G. Mehta
Keyword(s):  
Acetic Acid ◽  
Schiff Base ◽  
Antifungal Activity ◽  
Glycolic Acid ◽  
Acetyl Chloride ◽  
Aromatic Aldehydes ◽  
Cyclocondensation Reaction ◽  
Derivatives Of

2-Amino-6-(2-naphthalenyl)thiazolo[3,2-d]thiadiazole [1] was prepared by treatment of KCNS and Br2on 2-Amino-4-(2-naphthalenyl) thiazole. This amine on facile condensation with aromatic aldehydes afford Schiff Base/anils/azomethines(2a-h). These anils on cyclocondensation reaction with chloro acetyl chloride and thio glycolic acid (i.e. mercapto acetic acid) afford 2-azetidinones and 4-thiazolidinones respectively. The prepared compounds have been screened on some stains of fungai.

scholarly journals Synthesis of Novel Azetidinone and Thiazolidinones Derivatives and Evaluation of Their Antimicrobial Efficacy

2006 ◽  
Vol 3 (2) ◽  
pp. 103-109 ◽  
Author(s):  
K. H. Patel ◽  
A. G. Mehta
Keyword(s):  
Acetic Acid ◽  
Schiff Base ◽  
Glycolic Acid ◽  
Acetyl Chloride ◽  
Aromatic Aldehydes ◽  
Antimicrobial Efficacy ◽  
Cyclocondensation Reaction

2-Amino-4-(2-naphthalenyl) thiazole (1) was prepared from 2-acetylnapthalene. This amine on facile condensation with aromatic aldehydes afford Schiff Base/anils/azomethines(2a-h). These anils on cyclocondensation reaction with chloro acetyl chloride and thio glycolic acid (i.e. mercapto acetic acid) yields 2-azetidinones and 4-thiazolidinones respectively. The prepared compounds have been screened on some stains of bacteria.

scholarly journals Synthesis and Biological Activity of 3-Chloro-1-(4-perimidine methylcarbonylamino)-4-phenyl-azetidin-2-one

2009 ◽  
Vol 6 (s1) ◽  
pp. S91-S96 ◽  
Author(s):  
Dinesh R. Panchasara ◽  
Subhash Pande
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Schiff Base ◽  
Good Yield ◽  
Acetyl Chloride ◽  
Acid Hydrazide ◽  
Aromatic Aldehydes ◽  
Antibacterial And Antifungal Activities ◽  
Schiff Base Derivatives ◽  
Antibacterial And Antifungal

Perimidine-1-acetic acid hydrazide (1) undergoes facile condensation with aromatic aldehydes to afford the corresponding azomethine (i.e. Schiff base) derivatives (2a-h) in good yield. Cyclocondensation of compounds (2a-h) with chloro acetyl chloride affords 3-chloro-1-(4-perimidine methylcarbonylamino)-4-phenyl-azetidin-2-ones (3a-h). The structures of these compounds were established on the basis of analytical and spectral data. The newly synthesized compounds were evaluated for their antibacterial and antifungal activities.

scholarly journals The first in situ synthesis of 1,3-dioxan-5-one derivatives and their direct use in Claisen-Schmidt reactions

2019 ◽  
Vol 25 (1) ◽  
pp. 85-90 ◽  
Author(s):  
M. Javad Poursharifi ◽  
Mohammad M. Mojtahedi ◽  
M. Saeed Abaee ◽  
Mohammad M. Hashemi
Keyword(s):  
Acetic Acid ◽  
Aromatic Aldehydes ◽  
In Situ Synthesis ◽  
Stepwise Procedures ◽  
Time Periods ◽  
High Yields ◽  
Short Time ◽  
Direct Use ◽  
Derivatives Of

AbstractA method is developed for in situ generation of 1,3-dioxan-5-one derivatives 2. These compounds are simple precursors for accessing carbohydrate structures and previously had to be produced via stepwise procedures using excessive amounts of reagents. In the present work, three different derivatives of 2 were synthesized via the reaction of trialkoxyalkanes with dihydroxyacetone dimer 1 in the presence of acetic acid as the catalyst. In the same pot, derivatives of 2 were reacted with aromatic aldehydes and 30 mol% of pyrrolidine to obtain high yields of the respective bischalcones 3 within short time periods.

scholarly journals Synthesis and antimicrobial screening of pyrano[3,2-c]chromene derivatives of 1H-pyrazoles

2011 ◽  
Vol 9 (4) ◽  
pp. 635-647 ◽  
Author(s):  
Chetan Sangani ◽  
Divyesh Mungra ◽  
Manish Patel ◽  
Ranjan Patel
Keyword(s):  
Antifungal Activity ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Fungal Pathogens ◽  
Broth Microdilution ◽  
One Pot ◽  
E Coli ◽  
Cyclocondensation Reaction ◽  
Ft Ir ◽  
Derivatives Of

AbstractA new series of twenty four derivatives of pyrano[3,2-c]chromene IVa-x bearing 1H-pyrazole were synthesized by a one pot, base-catalyzed cyclocondensation reaction of 1H-pyrazole-4-carbaldehyde Ia-l, malononitrile II and 4-hydroxycoumarin IIIa-b. All the synthesized compounds were characterized by elemental analysis, FT-IR, 1H NMR and 13C NMR spectral data. All the synthesized compounds were screened against six bacterial pathogens, namely B. subtilis, C. tetani, S. pneumoniae, S. typhi, V. cholerae, E. coli and for antifungal activity against two fungal pathogens, A. fumigatus and C. albicans using the broth microdilution MIC method. Some of the compounds were found to be equipotent or more potent than commercial drugs against most of employed strains, as evident from the screening data.

Hot-Tube Reactions of Dehydroabietic Acid with Ketene-Producing Reagents. Pyrolysis of the Acid Chloride and Symmetrical and Mixed Anhydride Derivatives of Dehydroabietic Acid

1973 ◽  
Vol 51 (19) ◽  
pp. 3236-3241 ◽  
Author(s):  
Ray F. Severson ◽  
Walter H. Schuller
Keyword(s):  
Acetic Acid ◽  
Acetic Anhydride ◽  
Acid Chloride ◽  
Acetyl Chloride ◽  
Dehydroabietic Acid ◽  
Mixed Anhydride ◽  
Temperature Range ◽  
Acid Isomerization ◽  
Derivatives Of ◽  
Isopropenyl Acetate

Dehydroabietic acid (1a) was reacted with diketene, acetic acid, acetic anhydride, isopropenyl acetate, acetyl chloride, and acetone on Vycor rod at 450 °C in a hot tube. Dehydroabietic anhydride (1b) and acetyl dehydroabietate (1c) were pyrolyzed at 450 °C and dehydroabietyl chloride (1d) was pyrolyzed over a temperature range of 290–500 °C. The major olefin products resulting from decarboxylation of the various derivatives were 19-norabieta-4,8,11,13-tetraene (2), 19-norabieta-4(18),8,11,13-tetraene (3), 19-norabieta-3,8,11,13-tetraene (4), and cis-1,10a-dimethyl-7-isopropyl-1,2,3,9,10,10a-hexahydrophenanthrene (5). High conversions to these compounds were obtained. In the presence of the ketene-producing reagents the olefins were oxidized to yield substantial amounts of retene (6), compounds 2 and 5 being the most readily dehydrogenated. The acid isomerization of 2, 3, 4, and 5 was studied using p-toluenesulfonic acid in toluene at 110 °C.

scholarly journals XX. On some compounds and derivatives of acid

1863 ◽  
Vol 153 ◽  
pp. 437-452
Keyword(s):  
Inorganic Chemistry ◽  
Acetic Acid ◽  
Oxalic Acid ◽  
Sulphuric Acid ◽  
Glycolic Acid ◽  
Glyoxylic Acid ◽  
Careful Study ◽  
Organic Substances ◽  
Derivatives Of

Organic substances of simple composition, like marsh-gas, ethylene, alcohol, and acetic acid, are deserving of most careful study, not merely on account of their being repre­sentative members of numerous and important classes of bodies, but also because they form connecting links between the compounds of inorganic chemistry and the more complicated forms of organic nature. Glyoxylic acid belongs to this class of bodies, because it bears the same relation to oxalic acid that sulphurous acid does to sulphuric acid, and because it stands to glycolic acid as common aldehyde, C 2 H 4 O, does to alcohol, C 2 H 6 O. These relations suggested the experiments which will be described in the following pages.

scholarly journals Synthesis and Characterization of 3 - Substituted Coumarin

2016 ◽  
Vol 13 (1) ◽  
pp. 89-96
Author(s):  
Baghdad Science Journal
Keyword(s):  
Acetic Acid ◽  
Schiff Bases ◽  
1H Nmr ◽  
Acetyl Chloride ◽  
Aromatic Aldehydes ◽  
Synthesis And Characterization ◽  
Carbonyl Chloride ◽  
Ft Ir

The reaction of(2-oxo-2H-chromen-3-Carbonyl chloride)(k1) with hydrazine in boiling ethanol gives the hydrazide(K2).When compound (k2) reacts with various aromatic aldehydes ,the corres ponding Schiff bases(k3–k4) achieve new series of thiazotidines (k5–k6) and azetidinones (k7–k8) obtained from the reactions of appropriate Schiff bases with mercapto acetic acid and chloro acetyl chloride respectively. All the compounds are characterized by FT-IR,1H-NMR and GC-Ms.

scholarly journals Synthesis of 4,5-dihydro-1H-pyrazole derivatives based on 3-acetyl-5-nitropyridines

2021 ◽  
Author(s):  
Alena Stalinskaya ◽  
Daria Weber ◽  
Tulegen Seilkhanov ◽  
Ivan Kulakov
Keyword(s):  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
Aromatic Aldehydes ◽  
Pyrazole Derivatives ◽  
Crotonic Condensation ◽  
Derivatives Of

Abstract Claisen-Schmidt-type aldol-crotonic condensation of 3-acetyl-5-nitropyridine derivatives with various aromatic aldehydes was used for the preparation of pyridylchalcones. Cyclization of the latter with hydrazine hydrate in acetic acid afforded the corresponding N-acetyl derivatives of 4,5-dihydro-1H-pyrazole.

Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans

2019 ◽  
Vol 15 (6) ◽  
pp. 648-658 ◽  
Author(s):  
Manzoor Ahmad Malik ◽  
Shabir Ahmad Lone ◽  
Parveez Gull ◽  
Ovas Ahmad Dar ◽  
Mohmmad Younus Wani ◽  
...  
Keyword(s):  
Schiff Base ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Fungal Infections ◽  
Total Sterol ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Ergosterol Biosynthesis ◽  
Dependent Manner ◽  
Schiff Base Derivatives

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but also alternative treatment strategies are promptly required. Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. In this study, we synthesized some non-azole Schiff-base derivatives and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drugs- fluconazole (FLC) and amphotericin B (AmB) against four drug susceptible, three FLC resistant and three AmB resistant clinically isolated Candida albicans strains. To further analyze the mechanism of antifungal action of these compounds, we quantified total sterol contents in FLC-susceptible and resistant C. albicans isolates. Results: A pyrimidine ring-containing derivative SB5 showed the most potent antifungal activity against all the tested strains. After combining these compounds with FLC and AmB, 76% combinations were either synergistic or additive while as the rest of the combinations were indifferent. Interestingly, none of the combinations was antagonistic, either with FLC or AmB. Results interpreted from fractional inhibitory concentration index (FICI) and isobolograms revealed 4-10-fold reduction in MIC values for synergistic combinations. These compounds also inhibit ergosterol biosynthesis in a concentration-dependent manner, supported by the results from docking studies. Conclusion: The results of the studies conducted advocate the potential of these compounds as new antifungal drugs. However, further studies are required to understand the other mechanisms and in vivo efficacy and toxicity of these compounds.

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