scholarly journals Synthesis, Spectral and Microbial Studies of Some Novel Schiff Base Derivatives of 4-Methylpyridin-2-amine

2009 ◽  
Vol 6 (4) ◽  
pp. 1205-1210 ◽  
Author(s):  
J. J. Vora ◽  
S. B. Vasava ◽  
K. C. Parmar ◽  
S. K. Chauhan ◽  
S. S. Sharma
Keyword(s):  
Schiff Base ◽  
Antimicrobial Activities ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Acid Catalyzed ◽  
Derivatives Of ◽  
Broth Dilution

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.

scholarly journals Synthesis and Spectroscopic and Antimicrobial Studies of Schiff Base Metal Complexes Derived from 2-Hydroxy-3-methoxy-5-nitrobenzaldehyde

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
K. R. Joshi ◽  
A. J. Rojivadiya ◽  
J. H. Pandya
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Dilution Method ◽  
Aspergillus Clavatus ◽  
Schiff Base Ligands ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antimicrobial Studies ◽  
Schiff Base Metal Complexes ◽  
Broth Dilution

Two new series of copper(II) and nickel(II) complexes with two new Schiff base ligands 2-((2,4-dimethylphenylimino)methyl)-6-methoxy-4-nitrophenol and 2-((3,4-difluorophenylimino)methyl)-6-methoxy-4-nitrophenol have been prepared. The Schiff base ligands were synthesized by the condensation of 2-hydroxy-3-methoxy-5-nitrobenzaldehyde with 2,4-dimethylaniline or 3,4-difluoroaniline. The ligands and their metal complexes have been characterized by IR, 1H NMR, mass and electronic spectra and TG analysis. The Schiff base ligands and their metal complexes were tested for antimicrobial activity against Gram positive bacteria Staphylococcus aureus, and Streptococcus pyogenes and Gram negative bacteria Escherichia coli, and Pseudomonas aeruginosa and fungus Candida albicans, Aspergillus niger, and Aspergillus clavatus using Broth Dilution Method.

scholarly journals Synthesis and Bio-Evaluation of Novel N-(4-(8-Methoxy-2-Oxo-2H-Chromen-3-Yl) Thiazol-2-Yl) Amide Derivatives

2016 ◽  
Vol 71 ◽  
pp. 19-28
Author(s):  
Nilay Shah ◽  
Pineshkumar N. Patel ◽  
Dhanji Rajani ◽  
Denish C. Karia
Keyword(s):  
Acid Chloride ◽  
Antimalarial Activity ◽  
Mass Spectral ◽  
H Nmr ◽  
Chemical Structures ◽  
Compound C ◽  
Amide Derivatives ◽  
Ft Ir ◽  
Derivatives Of ◽  
Solvent Free Reaction

In present work, novel derivatives of substituted N-(4-(8-methoxy-2-oxo-2H-chromen-3-yl) thiazol-2-yl) amide have been synthesized. The solvent free reaction of 2-Hydroxy-3-methoxybenzaldehyde with Ethyl acetoacetate in presence of Piperidine catalyst produces 3-acetyl-8-methoxy-2H-chromen-2-one (C). Compound C was α- brominated using CuBr2and subsequently cyclized using Thiourea to produce 3-(2-aminothiazol-4-yl)-8-methoxy-2H-chromen-2-one as main scaffold (E). This scaffold E was finally reacted with different Acid chloride to isolate title compound derivatives. The chemical structures of synthesized compounds were confirmed by1H-NMR, FT-IR and Mass spectral/LCMS analysis. The synthesized compounds were screened for potential Antimicrobial, Antifungal and Antimalarial activity.

scholarly journals Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

2016 ◽  
Vol 69 ◽  
pp. 42-48
Author(s):  
Pineshkumar N. Patel ◽  
Denish C. Karia
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Glacial Acetic Acid ◽  
Mixed Solvent ◽  
Dilution Method ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Broth Dilution ◽  
C Nmr

Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin.

scholarly journals Synthesis and Antimicrobial Studies of Pyrimidine Pyrazole Heterocycles

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Rakesh Kumar ◽  
Jyoti Arora ◽  
Sonam Ruhil ◽  
Neetu Phougat ◽  
Anil K. Chhillar ◽  
...  
Keyword(s):  
Genetic Material ◽  
Oxidative Cyclization ◽  
Antifungal Drugs ◽  
Mass Spectral ◽  
H Nmr ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Derivatives Of

Prompted from the diversity of the wider use and being an integral part of genetic material, an effort was made to synthesize pyrimidine pyrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with satisfactory yield and purity. A novel series of 1,3-dimethyl-6-hydroxy-2,4-dioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5a–d) and 1,3-diaryl-6-hydroxy-4-oxo-2-thioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5e–l) has been synthesized. The structures of these compounds were established on the basis of FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. All the synthesized compounds were screened for their antimicrobial activity against bacteria and fungi. Among all the compounds, 5g was found to be the most active as its MIC was 31.25 µg/mL against S. aureus and B. cereus. The compounds 5h, 5c, and 5e also possess antibacterial activity with MIC values as 62.50, 125.00, and 500.00 µg/mL, respectively. The compounds 5c and 5j were found to have antifungal activity against Aspergillus spp. As antifungal drugs lag behind the antibacterial drugs, therefore we tried in vitro combination of these two compounds with standard antifungal drugs (polyene and azole) against Aspergillus spp. The combination of ketoconazole with 5c and 5j showed synergy at 1 : 8 (6.25 : 50.00 µg/mL) and 1 : 4 (25 : 100 µg/mL) against A. fumigatus (ITCC 4517) and A. fumigatus (VPCI 190/96), respectively.

scholarly journals Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2696 ◽  
Author(s):  
Teran ◽  
Guevara ◽  
Mora ◽  
Dobronski ◽  
Barreiro-Costa ◽  
...  
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Drug Candidates ◽  
Development Of Resistance ◽  
Schiff Base Derivatives ◽  
Wide Range ◽  
Derivatives Of

Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded.

scholarly journals An Efficient and Clean Synthesis of Thiophenyl Thiazole Depended Novel Triazolo[4,3-a]Quinoxaline Derivatives

2015 ◽  
Vol 51 ◽  
pp. 125-134
Author(s):  
Haresh G. Kathrotiya ◽  
Sagar P. Gami ◽  
Yogesh T. Naliapara
Keyword(s):  
Schiff Base ◽  
Elemental Analysis ◽  
Room Temperature ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Clean Synthesis ◽  
Quinoxaline Derivatives ◽  
Ft Ir ◽  
C Nmr

A simple and efficient approach for the synthesis of thiophenyl thiazole based triazolo [4,3-a] quinoxaline derivatives is described. In this methodology, 3-hydrazinyl-N-(4-(thiophen-2-yl) thiazol-2-yl) quinoxalin-2-amine derivatives treated with various aromatic aldehyde to form Schiff base which on treatment with iodobenzene diacetate in dichloromethane at room temperature to furnish title compounds. The synthesized compounds were characterized by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data

scholarly journals Synthesis of novel Schiff base derivatives of tacrine and investigation of their acetylcholinesterase inhibition potency

2019 ◽  
Vol 38 (1) ◽  
pp. 75 ◽  
Author(s):  
Elif Koyuncu ◽  
Ahmet Yaşar ◽  
Fatma Arslan ◽  
Nurşen Sari
Keyword(s):  
Schiff Base ◽  
Potent Inhibitor ◽  
Water Soluble ◽  
Acetylcholinesterase Inhibition ◽  
Ache Inhibitor ◽  
Schiff Base Derivatives ◽  
Ic50 Value ◽  
Ft Ir ◽  
Inhibition Potency ◽  
Derivatives Of

Investigation of acetylcholinesterase (AChE) inhibition potency of some new Schiff base derivatives of tacrine (9-amino-1,2,3,4-tetrahydroacridine) was reported in this paper. Novel Schiff base derivatives of tacrine (3a–g) have been synthesized, and they have been characterized by several methods (FT-IR, 1H-NMR, 13C-NMR, etc.). Then, inhibition effects on AChE by the synthesized compounds have been investigated by the spectrophotometric Ellman method. IC50, Ki, KM and Vmax values and inhibition types have been determined. It was seen that all compounds had the property of a water-soluble reversible AChE inhibitor. Structure 3a was found to be the most potent inhibitor, with the IC50 value of 22.1 ± 1.11  nM (tacrine's IC50 value was calculated as 34.1 nM).

scholarly journals Synthesis and Evaluation of Schiff Bases of 4-Amino-5-(chlorine substituted phenyl)-4H-1,2,4-triazole-3-thione as Antimicrobial Agents

2020 ◽  
Vol 41 (1) ◽  
pp. 26-35
Author(s):  
Kishor Devkota ◽  
Govinda Pathak ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Spectral Techniques ◽  
Schiff Base Derivatives ◽  
Bacteria And Fungi ◽  
Different Strains

Triazole ring system has attracted a continuously growing interest of synthetic organic chemists and those dealing with the medicinal compounds due to its versatile potential to interact with biological systems. Schiff bases are also considered as one of the most biologically active compounds.  The aim of the present study was to synthesize new Schiff bases bearing triazole nucleus and to assess their antimicrobial activities. Four new Schiff base derivatives of 1,2,4-triazole-3-thione were synthesized by combining two different pharmacophores viz. triazole nucleus and Schiff base moiety and were characterized by spectral techniques (UV, FT-IR, and NMR). The Schiff bases were evaluated for antibacterial (Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae) and antifungal (Candida albicans) activities. The synthesized compounds exhibited good to moderate activities against different strains of bacteria and fungi tested.

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