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

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.

2006 ◽  
Vol 3 (2) ◽  
pp. 103-109 ◽  
Author(s):  
K. H. Patel ◽  
A. G. Mehta

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.


2010 ◽  
Vol 7 (4) ◽  
pp. 1484-1490
Author(s):  
M. C. Patel ◽  
Dhameliya

5-((1, 3-Dioxoisoindolin-2-yl)methyl-2-hydroxybenzohydrazide (1) undergoes facile condensation with aromatic aldehydes to afford the correspondingN'-substituted-phenyl-5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxybenzohydrazide (2a-h) in good yields. Cyclocondensation of compounds (2a-h) with thioglycolic acid yields 5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxy-N-(4-oxo-2-substituted phenylthiazolidin-3-yl)benzamide (3a-h). These (3a-h) compounds were further reacted with benzaldehyde in the presence of sodium ethanolate affords, (Z) –N-(5-benzylidene-4-oxo-2-substituted phenyl-thiazolidin-3-yl)-5-((1,3-dioxoisoindolin-2-yl)methyl)-2-hydroxybenzamdie(4a-h). The structures of these compounds were established on the basis of analytical and spectral data. All the newly synthesized compounds were evaluated for their antibacterial and antifungal activities.


2006 ◽  
Vol 3 (4) ◽  
pp. 267-273 ◽  
Author(s):  
K. H. Patel ◽  
A. G. Mehta

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.


2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu

Abstract Thio-Schiff bases are becoming increasingly widespread in various branches such as the preparation of certain medicines, cosmetic products, and polymer production. In particular, the presence of antibacterial, antifungal, antiviral, antitumor and antimalarial properties of Schiff bases containing sulfur in the structure has made these compounds attractive in different disciplines. In this study, different derivatives of dimeric disulfide-Schiff bases have been synthesized. The antibacterial and antifungal activities of the synthesized these compounds were investigated in vitro against some human pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans, C. tropicalis, C. guilliermondii and C. glabrata). Test microorganisms were isolated from the patients appyling to Medical Faculty Hospital of Duzce University were used. Diffusion method was used to determine the antimicrobial activities of the compounds.standard antibacterial (Cefotaxime, Amoxicillin/clavulanicacid) and antifungal (Posaconazole) antibiotics were used as the control group and the results were compared. The result indicated that antimicrobial activity of Disulphide-Schiff Base Derivatives exhibited less activity against bacteria as compared to AMC30 (Amoxicillin/clavulanicacid), but highly effective against bacteria as compared to CTX30 (Cefotaxime). In addition, the compounds exhibited less activity against yeast.


2013 ◽  
Vol 11 (01) ◽  
pp. 37-39
Author(s):  
Rawaa Neamah ◽  
Shaimaa Adnan

In This study We are synthesis and characterization of some Schiff base and β- lactam derivatives) by three steps. The First react 2-amino-4-Chloro-6-methyl pyrimidine with 4-amino acetophenone in an acid medium to get shiff base derivative(E)-4-(1-((4-Chloro-6-methyl pyridine-2-yl)imino)ethyl)aniline (1), the second step (1) react with (3,4- dimethoxybenzal dehyde,4-methyl benzaldehyde,4-dimethylamino benzaldehyde,4-bromo benzaldehyde,4–hydroxy benzaldehyde, 4-Nitro benzaldehyde) to get Schiff base derivatives (2-7), the last step (2-7) derivatives react with Chloro acetyl chloride to get –β-lactam derivatives.(8-13) All these compounds are characterization by (FTIR), (1 H-NMR),(13C- NMR). After that study, the biological activity for all these derivatives to word two kinds of bacteria study the Enzymatic and Cancer Cell.


2016 ◽  
Vol 71 (7) ◽  
pp. 803-810 ◽  
Author(s):  
Mohamed E. Azab ◽  
Eman M. Flefel ◽  
Nermien M. Sabry ◽  
Abd El-Galil E. Amr

AbstractA series of tetracarboxamide and macrocyclic tripeptides have been prepared starting from 3,5-bis[N-(1-hydrazinyl-1-oxo-3-phenylpropan-2-yl)]pyridinecarboxamide 4 as starting material, which was synthesized from dinicotinic acid 1. Treatment of 4 with 1,4-diaminobutane, 1,6-diaminohexane, or cycloalkanone derivatives gave the corresponding macrocyclic tetracarboxamides (5a, b) and cycloalkyl hydrazone derivatives (6a–c), respectively. Additionally, the reaction of 4 with acetophenone or acetylpyridine derivatives gave the corresponding Schiff base derivatives 7a–e and 8a–c, respectively. Also, carboxylic acid hydrazide 4 was treated with acid anhydrides in glacial acetic acid to afford the corresponding diimide tetracarboxamide derivatives 9a, b, 10, and 11, respectively. The structures of newly synthesized compounds are established by physical and spectral data evidences. Some of the synthesized compounds were screened as antimicrobial agents.


Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2013 ◽  
Author(s):  
Ricardo Murcia ◽  
Sandra Leal ◽  
Martha Roa ◽  
Edgar Nagles ◽  
Alvaro Muñoz-Castro ◽  
...  

In this work, six complexes (2–7) of Cr(III) and Co(II) transition metals with triazole ligands were synthesized and characterized. In addition, a new ligand, 3,5-bis(1,2,4-triazol-1-ylmethyl)toluene (1), was synthesized and full characterized. The complexes were obtained as air-stable solids and characterized by melting point, electrical conductivity, thermogravimetric analysis, and Raman, infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that complexes 3–7 had 1:1 (M:L) stoichiometries and octahedral geometries, while 2 had a 1:2 (M:L) ratio, which was supported by DFT calculations. The complexes and their respective ligands were evaluated against bacterial and fungal strains with clinical relevance. All the complexes showed higher antibacterial and antifungal activities than the free ligands. The complexes were more active against fungi than against bacteria. The activities of the chromium complexes against Candida tropicalis are of great interest, as they showed minimum inhibitory concentration 50 (MIC50) values between 7.8 and 15.6 μg mL−1. Complexes 5 and 6 showed little effect on Vero cells, indicating that they are not cytotoxic. These results can provide an important platform for the design of new compounds with antibacterial and antifungal activities.


Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3250 ◽  
Author(s):  
Yahya Toubi ◽  
Farid Abrigach ◽  
Smaail Radi ◽  
Faiza Souna ◽  
Abdelkader Hakkou ◽  
...  

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins.


2010 ◽  
Vol 65 (5) ◽  
pp. 617-624 ◽  
Author(s):  
Prajwal L. Lobo ◽  
Boja Poojary ◽  
Kumsi Manjunatha ◽  
Nalilu Suchetha Kumari

A series of 2-(6-oxo-5,6-dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-Narylacetamides 6 were synthesized in good yield by condensing 5-aryloxymethyl-4H-1,2,4-triazole- 3-thiol 5 with various substituted N-phenyl-maleimides in acetic acid media. The newly synthesized compounds were characterized by spectral data and tested for their in vitro antibacterial and antifungal activity against a variety of microorganisms.


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