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, 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 Microwave-Assisted Synthesis of Schiff Bases of Isoniazid and Evaluation of Their Anti-Proliferative and Antibacterial Activities

Molbank ◽  
10.3390/m1189 ◽  
2021 ◽  
Vol 2021 (1) ◽  
pp. M1189
Author(s):  
Bayan Ahed Al-Hiyari ◽  
Ashok K. Shakya ◽  
Rajashri R. Naik ◽  
Sanaa Bardaweel
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Ic50 Values ◽  
In Vitro Inhibition ◽  
Mcf 7

Three new Schiff bases of isoniazid were synthesized using microwave-assisted synthesis and conventional condensation with aromatic aldehydes. Synthesized compounds were characterized using elemental analysis, IR, NMR, and Mass spectroscopy. Synthesized compounds were evaluated for antiproliferative activity against MCF-7 cell line. The IC50 values were from 125 to 276 µM. The compounds were also evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli. Results showed that the synthesized compounds produce significant antibacterial activity in vitro. Inhibition of compounds ranged from 13 to 18 mm.

Synthesis, Antimicrobial evaluation and Docking study of new Schiff bases of benzo[d]oxazol-5-amine derivatives.

2021 ◽  
pp. 4129-4136
Author(s):  
Nedaa A. Hameed A. Rahim ◽  
Sumayah Saadi Abbas ◽  
Sahar B. Aljuboori ◽  
Ammar A Razzak Mahmood
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Schiff Bases ◽  
Aromatic Aldehydes ◽  
Docking Study ◽  
Fungal Species ◽  
Active Centers ◽  
Molecular Docking Study ◽  
Gram Positive Bacteria

Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.

scholarly journals Synthesis and Bioinformatic Characterization of New Schiff Bases with Possible Applicability in Brain Disorders

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4160
Author(s):  
Speranta Avram ◽  
Ana Maria Udrea ◽  
Diana Camelia Nuta ◽  
Carmen Limban ◽  
Adrian Cosmin Balea ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Neurodegenerative Disorders ◽  
Aromatic Aldehydes ◽  
Brain Disorders ◽  
Ir And Nmr Spectroscopy ◽  
Bioinformatics Tools ◽  
Ft Ir ◽  
New Treatments ◽  
New Compounds

(1) Background: The research aims to find new treatments for neurodegenerative diseases, in particular, Alzheimer’s disease. (2) Methods: This article presents a bioinformatics and pathology study of new Schiff bases, (EZ)-N′-benzylidene-(2RS)-2-(6-chloro-9H-carbazol-2-yl)propanehydrazide derivatives, and aims to evaluate the drug-like, pharmacokinetic, pharmacodynamic and pharmacogenomic properties, as well as to predict the binding to therapeutic targets by applying bioinformatics, cheminformatics and computational pharmacological methods. (3) Results: We obtained these Schiff bases by condensing (2RS)-2-(6-chloro-9H-carbazol-2-yl)propanehydrazide with aromatic aldehydes, using the advantages of microwave irradiation. The newly synthesized compounds were characterized spectrally, using FT-IR and NMR spectroscopy, which confirmed their structure. Using bioinformatics tools, we noticed that all new compounds are drug-likeness features and may be proposed as potentially neuropsychiatric drugs (4) Conclusions: Using bioinformatics tools, we determined that the new compound 1e had a high potential to be used as a good candidate in neurodegenerative disorders treatment.

scholarly journals Green Chemistry Approach for Efficient Synthesis of Schiff Bases of Isatin Derivatives and Evaluation of Their Antibacterial Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jnyanaranjan Panda ◽  
V. Jagannath Patro ◽  
Biswa Mohan Sahoo ◽  
Jitendriya Mishra
Keyword(s):  
Green Chemistry ◽  
Schiff Bases ◽  
Reaction Times ◽  
Antibacterial Activities ◽  
Primary Amines ◽  
Microwave Assisted Synthesis ◽  
Azomethine Group ◽  
Microwave Assisted ◽  
Isatin Derivatives

Microwave-assisted organic synthesis, a green chemistry approach, is nowadays widely used in the drug synthesis. Microwave-assisted synthesis improves both throughput and turnaround time for medicinal chemists by offering the benefits of drastically reduced reaction times, increased yields, and pure products. Schiff bases are the important class of organic compounds due to their flexibility, and structural diversities due to the presence of azomethine group which is helpful for elucidating the mechanism of transformation and rasemination reaction in biological system. This novel compound could also act as valuable ligands for the development of new chemical entities. In the present work, some Schiff bases of Isatin derivatives was synthesized using microwave heating method. Schiff base of Isatin were synthesized by condensation of the keto group of Isatin with different aromatic primary amines. They were characterized by means of spectral data and subsequently subjected to the in vitro antibacterial activities against gram positive and gram negative strains of microbes. It was observed that the compound with electron withdrawing substituents exhibited good antibacterial activities against almost all the micro organisms.

scholarly journals In Vitro Antibacterial Activities of Aniline Dithiocarbamate Crystals with its Corresponding Oxovanadium(IV) and Zinc(II) Coordination Compounds

2018 ◽  
Author(s):  
Ayodele Odularu ◽  
Peter Adewale Ajibade ◽  
Albert Bolhuis
Keyword(s):  
Coordination Compounds ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
One Pot ◽  
Gram Negative ◽  
X Ray Crystallography ◽  
Mixed Ligands ◽  
Ft Ir ◽  
Modest Activity

Abstract Antibacterial activities can be improved using mixed ligands. Mixed ligands involved in this research are sodium sulfadiazine (Na-sfz) and dithiocarbamate (ai-dtc). One-pot synthesis was used to synthesize ligand of aniline dithiocarbamate (ai-dtc) and the corresponding coordination compounds of [VO(sfz)(ai-dtc)] and [Zn(sfz)(ai-dtc)]. Crystals of ai-dtc, which grew from the solution when refrigerated after five days, were diffracted with technique of single crystal x-ray crystallography to reveal the structure. Other characterization techniques involving physicochemical parameters, FT-IR, UV-Vis and NMR (1H NMR and 13C NMR) were carried out on ligands of ai-dtc, sfz and corresponding coordination compounds. Differences in results of FT-IR, UV-Vis and NMR between ligands and their respective metal ions confirmed the coordination. The in vitro antibacterial studies showed that the ligands (not the metal complexes) had modest activity against Gram negative bacteria: Staphylococcus aureus, whereas, the coordination compounds had modest activities against the Gram negative bacteria: Escherichia coli and Pseudomonas aeruginosa.

scholarly journals Indole-3-carbaldehyde Semicarbazone Derivatives: Synthesis, Characterization, and Antibacterial Activities

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Fernando Carrasco ◽  
Wilfredo Hernández ◽  
Oscar Chupayo ◽  
Celedonio M. Álvarez ◽  
Sandra Oramas-Royo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Antibacterial Activities ◽  
Isomeric Form ◽  
Bacterial Strains ◽  
H Nmr ◽  
Nmr Techniques ◽  
Ft Ir ◽  
Liquid Acetone

Four indole-3-carbaldehyde semicarbazone derivatives, 2-((5-bromo-1H-indol-3-yl)methylene)hydrazinecarboxamide (1), 2-((5-chloro-1H-indol-3-yl)methylene)hydrazinecarboxamide (2), 2-((5-methoxy-1H-indol-3-yl)methylene)hydrazinecarboxamide (3), and 2-((4-nitro-1H-indol-3-yl)methylene)hydrazinecarboxamide (4) were synthesized and characterized by ESI-MS and spectroscopic (FT-IR, 1H NMR, and 13C NMR) techniques. The two-dimensional NMR (in acetone-d6) spectral data revealed that the molecules 1 and 2 in solution are in the cisE isomeric form. This evidence is supported by DFT calculations at the B3LYP/6-311++G(d,p) level of theory where it was shown that the corresponding most stable conformers of the synthesized compounds have a cisE geometrical configuration, in both the gas and liquid (acetone and DMSO) phases. The in vitro antibacterial activity of compounds 1–4 was determined against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. Among all the tested semicarbazones, 1 and 2 exhibited similar inhibitory activities against Staphylococcus aureus (MIC = 100 and 150 μg/mL, respectively) and Bacillus subtilis (MIC = 100 and 150 μg/mL, respectively). On the other hand, 3 and 4 were relatively less active against the tested bacterial strains compared with 1, 2, and tetracycline.

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.

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