scholarly journals Synthesis, Characterization and Evaluate the Biological Activity of Novel Heterocyclic Derivatives from Azomethine Compounds

2019 ◽  
Vol 35 (4) ◽  
pp. 1360-1367
Author(s):  
Rasim Farraj Muslim ◽  
Suheb Eaid Saleh
Keyword(s):  
Biological Activity ◽  
Aromatic Amines ◽  
Aromatic Aldehydes ◽  
The Novel ◽  
Heterocyclic Derivatives ◽  
Primary Aromatic Amines ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Azomethine Compounds

This research includes synthesis of new seventh-membered heterocyclic derivatives as 1,3-oxazepine-dione derived from azomethine compounds. Azomethine compounds R1-R4 were synthesized by the reaction of aromatic aldehydes with primary aromatic amines. The novel of 1,3-oxazepine-dione derivatives R5-R9 were obtained from the treatment of azomethine compounds with anhydrides. The synthesized compounds were checked by TLC technique, spectral methods (FT-IR, H1-NMR) and measurements of some its physical properties. The biological activity of the heterocyclic derivatives was investigated against bacteria and fungi in vitro.

scholarly journals Synthesis of certain pyrrole derivatives as antimicro-bial agents

2009 ◽  
Vol 59 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Mosaad Mohamed ◽  
Ramdan El-Domany ◽  
Rania Abd El-Hameed
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Amines ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Pyrrole Derivatives ◽  
Gram Negative ◽  
Primary Aromatic Amines ◽  
Aryl Amines ◽  
Bacteria And Fungi

Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

scholarly journals SYNTHESIS, CHARACTERIZATION, AND STUDY THE BIOLOGICAL ACTIVITY OF SOME SCHIFF'S BASES, AND 1,3 - OXAZEPINE COMPOUNDS DERIVED FROM SULFAMETHOXAZOLE DRUG

2021 ◽  
Vol 13 (1) ◽  
pp. 43-54
Author(s):  
Enaam F. Mousa1 ◽  
Keyword(s):  
Biological Activity ◽  
Schiff Bases ◽  
Parent Drug ◽  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Fungal Species ◽  
Base Method ◽  
Ft Ir ◽  
Disk Method

This study including synthesis of some new Schiff bases compounds [1‐6] from the reaction of Sulfamethoxazole drug with some aromatic aldehydes in classical Schiff base method then treatment Schiff bases with succinic anhydride to get oxazepines rings [7-11]These derivatives were characterized by melting point, FT‐IR, 1H NMR and mass spectra. Some of synthesized compounds were evaluated in vitro for their antibacterial activities against three kinds of pathogenic strains Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa by agar diffusion disk method, and against the fungal species (Candida). The results showed that some of these derivatives have good antibacterial activities compared to biological activity of parent drug.

scholarly journals Synthesis and Bioassay of Novel Quinozolins

2019 ◽  
Vol 17 (72) ◽  
pp. 129-138
Author(s):  
Yasmine Kadom. Al-Majedy
Keyword(s):  
Twist Angle ◽  
Antimicrobial Properties ◽  
Heat Of Formation ◽  
Gram Negative Bacteria ◽  
The Novel ◽  
Gram Positive Bacteria ◽  
Visible Spectra ◽  
Ft Ir ◽  
Uv Visible

Novel Quinozolins were synthesized in a good yield through convert lacton to lactam and study the biological activity of the synthesized compounds. Quinozolins were characterized by elemental analysis, FT-IR and UV/visible spectra. The novel Quinozolins have been tested in vitro against (gram positive bacteria Staphylococcus aureus and against other gram negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus vulgaris; in order to assess their antimicrobial properties. Moreover, charge, bond length, bond angle, twist angle, heat of formation and steric energy were calculated by using of the ChemOffice program. The study indicates that these Quinozolins have high activity against tested bacteria. Based on the reported results, it may be concluded that the coumarin act as synthons for synthesis of new Quinozolins derivatives through the replacement of oxygen atom by nitrogen atom.

scholarly journals SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF NOVEL PYRAZOLO[3,4-b]PYRIDINES AND THEIR SPIRO-HETEROCYCLIC DERIVATIVES

2014 ◽  
Vol 10 (7) ◽  
pp. 2901-2915 ◽  
Author(s):  
Shawkat A. Abdelmohsen ◽  
Talaat I El Emary
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Aldehydes ◽  
Antibacterial And Antifungal Activity ◽  
Pyrimidine Derivatives ◽  
Spiro Derivatives ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
New Compounds ◽  
Hydrazone Derivative

The present work describes the synthesis of a novel series of heterocyclic moieties derived from 5-acetylpyrazolo[3,4-b]pyridine (1). The formation of chalcones (2a-d) was utilized to synthesize pyrazoline, isoxazoline and pyrimidine derivatives (3-10). Thiosemicarbazone and semicarbazone (11, 17) were utilized to synthesize other new triazolethiones, thiadiazole and selenadiazole derivatives (11-19). Some new spiro derivatives (22-25) were synthesized by the reaction of chalcone (21) of 1 and isatine with hydrazines, hydroxyl amines and thiourea. Also, The reaction of 1 with cyanoacetyl hydrazine gave the hydrazide-hydrazone derivative 26, which was allowed to react with aromatic aldehydes and α-cyanocinnamonitrile to afford coumarine and substituted pyridine derivatives (28, 29). The structures of all the new compounds have been established on the basis of their analytical and spectral data. Twenty two of the synthesized compounds were also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi and most are found to possess promising antimicrobial activity when compared with Chloramphenicol and Clotrimazole

scholarly journals Studies on Synthesis of Aldimines: Part-I. Synthesis, Characterization and Biological Activity of Aldimines from Benzaldehyde with variedly substituted anilines

2018 ◽  
Author(s):  
C. J. Patil ◽  
Manisha C. Patil ◽  
Mrunmayee C. Patil
Keyword(s):  
Biological Activity ◽  
Aromatic Aldehyde ◽  
Elemental Analysis ◽  
High Purity ◽  
Aromatic Amines ◽  
Condensation Reaction ◽  
Physical Constant ◽  
High Yield ◽  
Substituted Anilines

A conventional condensation reaction of an aromatic aldehyde, Benzaldehyde with seven different aromatic amines viz. Aniline, 2-Choro-aniline, 3-Choro-aniline, 4-Choro-aniline, 2-Nitro-aniline, 3-Nitro-aniline and 4-Nitro-aniline and reacted efficiently to synthesize a series of Aldmines, I to VII, in moderate to high yield and high purity. The reaction was monitored and the products were analyzed by employing the TLC technique. All the products obtained were characterized by their colour, physical constant, TLC, elemental analysis and spectral (UV-Vis and FTIR) method. The synthesized Aldimines were subjected to in vitro biological activity.

Synthesis, admetSAR predictions, DPPH radical scavenging activity and potent anti-mycobacterial studies of hydrazones of substituted 4-(anilinomethyl)benzohydrazides (Part 2)

2020 ◽  
Vol 16 ◽  
Author(s):  
Vijay J. Desale ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Aromatic Aldehydes ◽  
Spectroscopic Characterization ◽  
Common Infectious Disease ◽  
In Silico Admet ◽  
Ft Ir ◽  
Mycobacteria Tuberculosis ◽  
Dpph Radical Scavenging

Background: For the past several decades, we are remarking presence of the tuberculosis (TB) as the most common infectious disease leading mortality.and antimicrobial, etc. Objective: Hydrazone containing azometine group (-NHN=CH-) compounds has been reported for broad range of bioactivities such as antiplatelet, analgesic, antiinflammatory, anticonvulsant, antidepressant, antimalarial, vasodilator , antiviral and antimicrobial, etc. Method: For synthesis of our compounds (4a-4d) and (6a-6e), we have treated aromatic amines with methyl terephthalaldehydate in methanol giving us Schiff’s bases followed by reductive amination and further treatment with hydrazine hydrate to give acid hydrazides (4a-4d). These acid hydrazides were then treated with different aromatic aldehydes to yield hydrazones (6a-6d). All our synthesized compounds were subjected to FT-IR, NMR, and UV spectroscopic characterization. Results: Compounds (4a-4d) and (6a-6e) were found to have highly potent activity against Mycobacteria tuberculosis (Vaccine strain, H37 RV strains): ATCC No- 27294 (MIC:1.6-6.25 μg/mL) than standard anti-TB drugs. Our compounds exhibited good radical scavenging potentials(0-69.2%) as checked from DPPH protocol. All compounds also demonstrated good in-silico ADMET results. Conclusion: Our current study revealed promising in-vitro antituberculosis and antioxidant profiles of hydrazidehydrazone analogues.

Cyclisation of 1-Phenyl-4-carboxymethylmercapto-5-arylazo-hydantoins

1981 ◽  
Vol 36 (4) ◽  
pp. 501-504 ◽  
Author(s):  
A. F. A. Shalaby ◽  
M. A. Abdel Aziz ◽  
S. S. M. Boghdadi
Keyword(s):  
Acetic Acid ◽  
Acetic Anhydride ◽  
Aromatic Amines ◽  
Sodium Acetate ◽  
Aromatic Aldehydes ◽  
Mannich Bases ◽  
Anhydrous Sodium Acetate ◽  
Primary Aromatic Amines ◽  
Hydantoin Derivatives

Abstract 1-Phenyl-4-carboxymethylmercapto-5-arylazo-hydantoin derivatives (3a-f) were cyclised with acetic anhydride to give the bicyclic products (4a-f). Compounds 4 a, b condensed with aromatic aldehydes in acetic acid and in presence of anhydrous sodium acetate yielding the corresponding arylidene derivatives (5a-c). Compounds 4a, b also couple with aryldiazonium salts to give the expected coloured arylazo compounds (6a-j). 4 a, b reacted with formaldehyde and primary aromatic amines in ethanol to give the corresponding Mannich bases (7a-f).

scholarly journals Synthesis, Characterization and in vitro Evaluation of 3-(4-(Methylthio)phenyl)-1-(thiophene-3-yl)prop-2-en-1-one

2021 ◽  
Vol 33 (5) ◽  
pp. 1077-1084
Author(s):  
Binkey Acharjee ◽  
E. Dhineshkumar ◽  
Debasis Bandyopadhyay ◽  
S. Srinivasan
Keyword(s):  
Energy Gap ◽  
Antioxidant Activities ◽  
Docking Studies ◽  
Partial Density ◽  
The Novel ◽  
Molecular Systems ◽  
Over Expression ◽  
Potential Map ◽  
Ft Ir

In present study, a novel 3-(4-(methylthio)phenyl)-1-(thiophene-3-yl)prop-2-en-1-one (1) was synthesized through the chalcone reaction. The FT-IR, 1H & 13C NMR and mass analysis, UV-visible and fluorescent spectroscopic system were utilized to characterize the synthesized compound. The charge density data was used to explain the characteristics of molecular systems. In addition, in the form of the complete and partial density of states, the HOMO-LUMO energy gap and electrostatic potential map, etc. and some quantum chemical insights have been obtained. Furthermore, to demonstrate the possible applications of thiophene-chalcone derivative (1) in nonlinear optics, the polarizability and first hyperpolarizability were measured. Molecular docking studies were also conducted in order to illustrate the over expression of estrogen receptor in 75% of 5J6A protein. The novel compound was tested for its anticancer and antioxidant activities of in vitro analyses. The substantial antioxidant activity was demonstrated by the newly synthesized compound 1.

scholarly journals Synthesis of New Nucleoside Analogues From Benzimidazole and Evaluation of Their Antimicrobial Activity

2016 ◽  
Vol 13 (2) ◽  
pp. 317-332
Author(s):  
Baghdad Science Journal
Keyword(s):  
Sodium Methoxide ◽  
Aromatic Aldehydes ◽  
Nucleoside Analogues ◽  
Prepared Compound ◽  
Gram Negative ◽  
Ft Ir ◽  
Anomeric Carbon ◽  
Base Moiety ◽  
Ft Ir Spectroscopy

Our goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified by FT-IR Spectroscopy and some of them with H1 –NMR and C13-NMR Spectroscopy. The synthesized nucleoside analogues were screened for their antibacterial activity in vitro against four types of bacteria including, Bacillus Staphylococcus, aureus (Gram Positive), E.Coli and Pseudoman as (Gram Negative).Also were screened against four types of Fungi (Aspergines flurs, Aspergillus fumgntnts, Aspergillus niger and pencillum).

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