scholarly journals Synthesis of Some New Azetidinone Derivatives Containing Aryl Sulfonyloxy Group

2004 ◽  
Vol 1 (4) ◽  
pp. 194-198
Author(s):  
H. S. Patel ◽  
H. D. Desai
Keyword(s):  
Sodium Salt ◽  
Acetyl Chloride ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Schiff’S Bases ◽  
Aniline Derivative ◽  
Schiff's Bases

Some novel azetidinone derivatives containing aryl sulfonyloxy group have been prepared. The 4-sulfonyloxy aniline derivative (2) has been prepared by reaction of 4-nitro phenol (sodium salt) with N-acetyl sulfanilyl chloride (ASC) followed by hydrolysis by ethanolic HCl. This compound (2) undergoes facile condensation reaction with aromatic aldehydes to yield different Schiff’s bases (3a-h). Cyclocondensation of compounds (3a-h) with chloro acetyl chloride yields different 2-azetidinone derivatives (4a-h).

Green Synthesis, Characterization, DPPH and Ferrous Ion-chelating (FIC) Activity of Tetrakis-Schiff’s Bases of Terephthalaldehyde

2019 ◽  
Vol 16 (3) ◽  
pp. 249-255
Author(s):  
Momin Khan ◽  
Umar Ali ◽  
Anis Ur Rahman ◽  
Muhammad Ibrahim ◽  
Abdul Hameed ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Aromatic Aldehydes ◽  
Ferrous Ion ◽  
Future Research ◽  
Scavenging Activity ◽  
Schiff’S Bases ◽  
Schiff's Bases ◽  
Antioxidant Agents

Background: The role of small molecules as antioxidants to prevent the oxidation of other molecules and inhibit them from radical formation is the area of much interest to cure disease especially cancer. Moreover, the antioxidants play important role as stabilizers to prevent oxidation of fuels and lubricants. </P><P> Methods: In the present study, fifteen tetrakis-Schiff’s bases derivatives (1-15) were synthesized and screened for their antioxidant activities. Compounds 1-15 were synthesized by continuous stirring of reaction mixture of 1,4-bis (hydrazonomethyl)benzene (1 mmol) with various substituted aromatic aldehydes (2 mmol) in distilled water using acetic acid as catalyst at room temperature for 2-10 min. </P><P> Results: Our present study showed that all compounds are better ferrous ion-chelating agents except compound 1,4-bis((E)-((E)-(3,4-dimethoxybenzylidene)hydrazono)methyl)benzene (6) (IC50 = 329.26 &#177; 4.75 &#181;M) which has slightly low activity than the standard EDTA (IC50 = 318.40 &#177; 5.53 μM). In addition, DPPH radical scavenging activity of eleven compounds showed higher activity than the standard. However, remaining four compounds showed comparable radical scavenging activity to the standard DPPH (IC50 = 257.77 &#177; 4.60 &#181;M). </P><P> Conclusion: The series of fifteen Schiff’s bases (1-15) were synthesized and evaluated as antioxidants. From both assays, it has been demonstrated that most of the tetrakis-Schiff’s bases have potential to serve as leads for the development of antioxidant agents for future research.

scholarly journals Synthesis, characterization and anti-bacterial activity of novel schiff bases of pyridin-3 yl-carbohydrazide derivatives

2021 ◽  
pp. 23-26
Author(s):  
Ravi Kumar Konda ◽  
Anish Kumar K ◽  
Phani Lakshman M ◽  
Mohammed Asif ◽  
Anusha Reddy D
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Schiff Bases ◽  
Wide Spectrum ◽  
Cyclic Compound ◽  
Aromatic Aldehydes ◽  
Bacterial Activity ◽  
Schiff’S Bases ◽  
Ethyl Nicotinate ◽  
Schiff's Bases

Heterocyclic compounds are cyclic compounds containing carbon and other heteroatoms. The most common heteroatoms are oxygen, nitrogen, and Sulphur. A heterocyclic compound is a cyclic compound that has atoms at least two different elements as members of its ring. A Schiff base (azomethine) is named after its inventor, Hugo Schiff and it is a functional group that contains a carbon-nitrogen double bond with the nitrogen atom connected to an aryl or alkyl group but not hydrogen. Schiff bases of Pyridin-3 yl-carbohydrazide derivatives from ethyl nicotinate and different aromatic aldehydes. Schiff’s bases are aromatic substituted imine compounds. These compounds are very important in the medicinal and pharmaceutical fields because of their wide spectrum of biological activity. Schiff’s bases show antibacterial activity, antifungal activity, and also antitumor activity. Aromatic aldehydes were refluxed with ethyl nicotinate using ethanol as a solvent to form Schiff's bases. All chemicals are taken in equimolar concentrations. The synthesized compounds were characterized by melting point, solubility, percentage yield, TLC, and IR spectral analysis. All derivatives are evaluated for anti-bacterial activity by the cup plate method. The antibacterial activity of test compounds was compared against standard Streptomycin. The 5 synthesized compounds show moderate antimicrobial activity. The experimental work summarizes the synthesis and in-vitro antibacterial activity of Schiff base derivatives.

scholarly journals Synthesis and Antimicrobial Activity of Some 1-arylideneamino-4-(4-chlorobenzylidene)-2-methyl- 1H-imidazolin-5(4H)-one Compounds

2019 ◽  
Vol 35 (2) ◽  
pp. 822-828
Author(s):  
Cong Tien Nguyen ◽  
Dao Thi Hong Dinh ◽  
Thin Van Nguyen ◽  
Giang Duc Le ◽  
Hien Cao Nguyen
Keyword(s):  
Antimicrobial Activity ◽  
Hydrazine Hydrate ◽  
Spectral Data ◽  
1H Nmr ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Gram Negative Bacteria ◽  
Schiff’S Bases ◽  
Gram Negative ◽  
Schiff's Bases

4-Chlorobenzylidene-2-methyl-(4H)-oxazol-5-one, which were prepared from 4-chlorobenzaldehyde and acetylglycine in reaction with hydrazine hydrate in ethanol gave 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one. However, treatment of 4-chlorobenzylidene-2-methyl-(4H)-oxazol-5-one with hydrazine hydrate in pyridine yielded 3-(4-chlorophenyl)propanohydrazide. Reaction of 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one with aromatic aldehydes gave eight corresponding Schiff’s bases namely 1-arylideneamino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-ones. The structure of the 3-(4-chlorophenyl)propanohydrazide and the imidazoline-5-one compounds was confirmed by IR, 1H-NMR and MS spectral data. The Schiff’s bases were tested for antimicrobial activities against several strains of Gram-positive, Gram-negative bacteria, molds and yeasts.

scholarly journals The synthesis and antimicrobial study of some azetidinone derivatives with the para-anisidine moiety

2007 ◽  
Vol 72 (5) ◽  
pp. 437-442 ◽  
Author(s):  
Ishwar Bhat ◽  
Sunil Chaithanya ◽  
P.D. Satyanarayana ◽  
Balakrishna Kalluraya
Keyword(s):  
1H Nmr ◽  
Spectroscopic Analysis ◽  
Aromatic Aldehydes ◽  
Chloroacetyl Chloride ◽  
Schiff’S Bases ◽  
Antimicrobial Study ◽  
Schiff's Bases ◽  
Agar Disc ◽  
Antifungal Potential ◽  
Antibacterial And Antifungal

Azetidinones were synthesized from p-anisidine in two steps. First the Schiff's bases were prepared by reacting the hydrazide of an anisidine derivative with different aromatic aldehydes. Cyclocondensation of the Schiff's bases with chloroacetyl chloride in the presence of triethylamine resulted in the formation of the corresponding azetidinone analogues. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR and mass spectroscopic analysis. The antibacterial and antifungal potential of the synthesized compounds were evaluated by the agar disc method.

Synthesis of 3-(Cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8- carboxylic Acids Via an Efficient Three-component Condensation Reaction between Cyclohexylisocyanide and 2-Aminopyridine-3-carboxylic Acid in the Presence of Aromatic Aldehyde

2018 ◽  
Vol 21 (4) ◽  
pp. 298-301 ◽  
Author(s):  
Ghasem Marandi
Keyword(s):  
Biological Sciences ◽  
Carboxylic Acid ◽  
Carboxylic Acids ◽  
High Performance ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
New Materials ◽  
One Pot ◽  
High Yields ◽  
Benzaldehyde Derivatives

Aim and Objective: The reaction of cyclohexylisocyanide and 2-aminopyridine-3- carboxylic acid in the presence of benzaldehyde derivatives in ethanol led to 3-(cyclohexylamino)-2- arylimidazo[1,2-a]pyridine-8-carboxylic acids in high yields. In a three component condensation reaction, isocyanide reacts with 2-aminopyridine-3-carboxylic acid and aromatic aldehydes without any prior activation. Material and Methods: The synthesized products have stable structures which have been characterized by IR, 1H, 13C and Mass spectroscopy as well as CHN-O analysis. Results: In continuation of our attempts to develop simple one-pot routes for the synthesis of 3- (cyclohexylamino)-2-arylimidazo[1,2-a]pyridine-8-carboxylic acids, aromatic aldehydes with divers substituted show a high performance. Conclusion: In conclusion, this study introduces the art of combinatorial chemistry using a simple one-pot procedure for the synthesis of new materials which are interesting compounds in medicinal and biological sciences.

DFT Study and Synthesis of Novel Bioactive Bispyrazole Using Mg/AlLDH as a Solid Base Catalyst

2020 ◽  
Vol 14 ◽  
Author(s):  
Soufiane Akhramez ◽  
Youness Achour ◽  
Mustapha Diba ◽  
Lahoucine Bahsis ◽  
Hajiba Ouchetto ◽  
...  
Keyword(s):  
Dft Calculations ◽  
Experimental Finding ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Mechanistic Study ◽  
Knoevenagel Reaction ◽  
Solid Base ◽  
Reaction Conditions ◽  
Aryl Aldehyde

Background: In this study, an efficient synthesis of novel bispyrazole heterocyclic molecules by condensation of substituted aromatic aldehydes with 1,3-diketo-N-phenylpyrazole by using Mg/Al-LDH as heterogeneous catalyst is reported. The attractive features of this protocol are as follows: mild reaction conditions, good yields and easiness of the catalyst separation from the reaction mixture. Further, a mechanistic study has been performed by using DFT calculations to explain the observed selectivity of the condensation reaction between aryl aldehyde and 1,3-diketo-N-phenylpyrazole via Knoevenagel reaction. The local electrophilicity/ nucleophilicity that allows explaining correctly the experimental finding. Methods: The bispyrazole derivatives 3a-m were prepared by condensation reaction of substituted aromatic aldehydes with 1,3-diketo-Nphenylpyrazole by using Mg/Al-LDH as heterogeneous catalyst under THF solvent at the refluxing temperature. Objective: To synthesize a novel bispyrazole heterocyclic molecule may be have important biological activities and thus can be good candidates for pharmaceutical applications. Results: This protocol describes the Synthesis of Bioactive Compounds under mild reaction conditions, good yields and easiness of the catalyst separation from the reaction mixture. Further, a mechanistic study has been performed by using DFT calculations to explain the observed selectivity of the condensation reaction between aryl aldehyde and 1,3-diketo-N-phenylpyrazole via Knoevenagel reaction. The local electrophilicity/ nucleophilicity that allows explaining correctly the experimental finding. Conclusion: In summary, the pharmacologically interesting bis-pyrazole derivatives have been synthesized through Mg/Al-LDH as a solid base catalyst, in THF as solvent. Thus, the synthesized bioactive compounds containing the pyrazole ring may be have important biological activities and thus can be good candidates for pharmaceutical applications. Therefore, the catalyst Mg/Al-LDH showed high catalytic activity. Besides, a series of bispyrazole molecules were synthesized with a good yield and easy separation of the catalyst by simple filtration. Moreover, DFT calculations and reactivity indexes are used to explain the selectivity of the condensation reaction between aryl benzaldehyde and 1,3-diketo-Nphenylpyrazole via Knoevenagel reaction, and the results are in good agreement with the experimental finding.

Synthesis of Schiff's bases Derived from 2- Amino - 1,3,4- Thiadiazole and 1,3,4- Oxadiazole with Naphthaldehydes

2006 ◽  
Vol 9 (1) ◽  
pp. 21-28
Author(s):  
Emaad . T. bakir Al-Takrity ◽  
◽  
Ibtisam K. Jassim ◽  
Wissam K. Jassim ◽  
◽  
...  
Keyword(s):  
Schiff’S Bases ◽  
Schiff's Bases
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