scholarly journals Synthesis , Characterization and Biological activity of new derivatives of Chromen-2-one

2018 ◽  
Vol 15 (1) ◽  
pp. 6130-6135
Author(s):  
Aziz Behrami

We report the organic syntheses of new derivatives  from Chromen-2-one and their  antibacterial activity. Compounds  4-[Acetyl-(2-oxo-2H-chromen-4-yl)-amino]- benzenesulfonyl chloride 1a, 4-[Acetyl-(2-oxo-3-phenylsulfamoyl-2H-chromen-4-yl)-amino]-benzenesulfonyl chloride 2a , 2-{4-[Acetyl-(4-chlorosulfonyl-phenyl)-amino]-2-oxo-3-phenylsulfamoyl-2H-chromen-7-ylamino}-benzoic acid  3a. All Structures have been synthesized and characterized using melting points , IR spectra , 1H-NMR, 13C-NMR spectra , and elemental analyses  . The purified synthesized compounds (1a,2a,3a), at contcentrations 2,3,5 mg/ml was tested for their  antibacterial activity against three bacterial cultures ;Staphylococcus aureus, Escherchia coli and Bacillus cereus. The antibacterial activity of synthesized compounds are compared with antibacterial activity of standard antibiotics cephalexine and streptomycine.   The compounds (1a,2a,3a) shows  different bacteriostatic and bacteriocidal activity.

2017 ◽  
Vol 12 (6) ◽  
pp. 4108-4111
Author(s):  
Aziz Behrami ◽  
Kozeta Vaso

In present paper , we report the organic syntheses of three compounds from 4-Amino-7-chloro -2-oxo-2H –chromen -3carbaldehyde and describe the results of antibacterial activity of purified compounds.7-Chloro-4-[(2-hydroxy-benzylidene)amino]-2-oxo-2H-chromen-3-carbaldehyde(1a).4-[(2-Hydroxy-benzylidene)-amino]-7-(4-hydroxy-phenylamino)-2-oxo-2Hchromen-3-carbaldehyde (2a) ,([4-[(2-Hydroxy-benzylidene)-amino]-7-(4-hydroxyl-phenylamino)-2-oxo-chromen-3ylmethylene]-amino)-acetic acid (3a),have been synthesized and characterized using melting points , IR spectra , 1H-NMR and 13C-NMR spectra. The antibacterial activity of synthesized compounds and streptomycin and cefalexine at concentractions of 2mg/ml, 3mg/ml and 5mg/ml , have been evaluated against three strains of bacterial culture; Staphylococcus aureus, E.coli and Bacillus cereus. The compounds show bacteriostatic and bactericidal activity.


2006 ◽  
Vol 60 (1) ◽  
Author(s):  
M. Deska ◽  
W. Śliwa

AbstractSynthesis of N-and C-substituted derivatives of benzo[h][1,6]naphthyridine, bearing 2-hydroxyethyl group has been made by quaternization reaction and by condensation of corresponding methylbenzonaphthyridines with formaldehyde. For six derivatives of isomeric benzo[c][1,5]-, benzo[h][1,6]-, and benzo[f][1,7]naphthyridines the 13C NMR spectra are discussed.For ten compounds the geometry was optimized with the AM1 and, in one case also with the ab initio 6–31G method; their effective charge values have also been calculated.


1976 ◽  
Vol 16 (4) ◽  
pp. 629-630
Author(s):  
V. I. Stanko ◽  
T. A. Babushkina

1947 ◽  
Vol 134 (877) ◽  
pp. 538-543 ◽  

A series of basic derivatives of cholane and norcholane has been examined for bacteriostatic activity against the Gram-positive Staphylococcus aureus and Lactobacillus helveticus and the Gram-negative Bacillus lactis aerogenes . The basic derivatives, in general, were more highly bacteriostatic against the Gram-positive organisms than against the Gram-negative. Of the compounds studied, the highest antibacterial activity was shown by 3:7:12-trihydroxy-23-guanido-norcholane hydrochloride. No relationship was apparent between the lowering of the surface tension of the medium induced by the compounds and their bacteriostatic activity.


1992 ◽  
Vol 237 ◽  
pp. 95-113 ◽  
Author(s):  
Nikolay E. Nifant'ev ◽  
Alexander S. Shashkov ◽  
Grigory M. Lipkind ◽  
Nikolay K. Kochetkov

Author(s):  
A. V. Zuraev ◽  
A. V. Lishai ◽  
Yu. V. Grigoriev ◽  
O. A. Ivashkevich

A number of 1,4- and 1,4,5-triazoles have been synthesized using a modified catalytic system for the Huisgen [3+2] cycloaddition reaction. The bactericidal activity of the synthesized compounds has been studied. The synthesized derivatives of 1H-1,2,3-triazoles have demonstrated higher antibacterial activities in relation to the pathogen Staphylococcus aureus strain which can be comparable with the clinically used antibiotic “Cefotaxime”.


2021 ◽  
Vol 68 (3) ◽  
pp. 567-574
Author(s):  
Guo-Xu He ◽  
Ling-Wei Xue

A series of three new hydrazone compounds derived from the condensation reactions of 4-dimethylaminobenzohydrazide with 4-dimethylaminobenzaldehyde, 2-chloro-5-nitrobenzaldehyde and 3-methoxybenzaldehyde, respectively, were prepared. The compounds were characterized by elemental analysis, infrared and UV-vis spectra, HRMS, 1H NMR and 13C NMR spectra, and single crystal X-ray diffraction. Crystals of the compounds are stabilized by hydrogen bonds. The compounds were assayed for antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus) and antifungal (Aspergillus niger and Candida albicans) activities by MTT method. The results indicated that compound 2 is an effective antibacterial material.


2019 ◽  
Vol 16 (3) ◽  
pp. 405-412 ◽  
Author(s):  
Ahmed A.O. Abeed ◽  
Talaat I. El-Emary ◽  
Mohamed S.K. Youssef

<p>Aim and Objective: This work presents the synthetic capability and the exploitation of 1,3-diphenyl- 1H-pyrazole-4-carboxladehyde 1 and 5-diphenyl pyrazolyl-2-pyrazoline analogue 8 to serve as excellent precursors for the synthesis of substituted indol-2,3-dione, trizolo[3,4-a]benzazoles, thiazolo[2,3- a]benzimidazole-3-one, substituted 2-pyrazoline and pyrazole-substituted-pyrazolines using various reagents. </P><P> Materials and Methods: Using chemicals from Aldrich, Fluka, or Merck, and pure solvents, we apply the synthetic procedures for the synthesis of novel heterocycles. The melting points of these compounds were determined using APP. Digital ST 15 melting point apparatus. SP3-100 spectrophotometer recorded FT-IR spectra (KBr) (cm-1). NMR spectra (&#948;, ppm) were recorded on 400 MHz AVANCE-III High-Performance FT-NMR Spectrometer BRUCKER (Switzerland) and some 1H NMR spectra were recorded on Varian EM-360L NMR Spectrophotometer (90 MHz) (USA) in CDCl3 or DMSO-d6 as a solvent. Elemental analyses were carried out at a Vario EL C, H, N, and S Analyzer. Bromine was determined using direct titration method after carius combustion. </P><P> Results: The structures of the compounds were confirmed by IR, 1H NMR, 13C NMR, and elemental analyses. </P><P> Conclusion: 1,3-Diphenyl-1H-pyrazole-4-carboxladehyde 1 and 2-pyrazoline derivative 9 confirmed their importance in the synthetic organic chemistry. Depending on the formyl group of aldehyde 1 and active methylene of pyrazoline 8, we synthesized new series of heterocycles; indol-2,3-dione, trizolo[3,4-a]benzazole, thiazolo[2,3-a]benzimidazole-3-one and pyrazolyl-pyrazoline derivatives expecting their pharmacological applications. The targeted compounds were substantiated from its spectral data.</p>


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