Synthesis and Characterizations of Oxazolo Pyrimidine Derivatives as Biological Active and Antiinfective Agents (original) (raw)
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Synthesis, Characterization and Antimicrobial Evaluation of Some Pyrimidine Derivatives
Zenodo (CERN European Organization for Nuclear Research), 2022
The main objective of present work is to synthesis, characterization, and evaluation of antimicrobial activity of some pyrimidine derivatives containing O, N, and S in the ring. Pyrimidine derivatives were prepared in three steps. In the i n i t i a l step, chalcones containing-NO2 functional group were synthesized using Claisen Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the next step,-NO2 group was reduced to-NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,Ndiisopropylethylamine to obtain pyrimidine derivatives. Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro. Pyrimidine derivatives were synthesized and purified using column chromatography. Purity of synthesized pyrimidines was determined by HPLC. Pyrimidines were characterized by different analysis such as elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines indicates the proposed structures. Finally antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives.
2016
Objectives: The objective of this work is to synthesize new pyrimidine derivatives starting from ethyl 2,4-dioxo-4-(thiophen-2-yl)butanoate. Several oxadiazole, triazole, and thiadiazole moieties were incorporated into the pyrimidine backbone. The structure of the novel compounds was characterized by elemental analysis and spectroscopic methods. Methods: Synthesis of the target compounds was materialized starting from 2-oxo-6-(thiophen-2-yl)-2,3-dihydropyrimidine-4-carbohydrazide (4) which was prepared from the appropriate ethyl 2-oxo-6-(thiophen-2-yl)-2,3-dihydropyrimidine-4-carboxylate (2). Several synthetic pathways were used for the preparation of the targets. Some of the newly synthesized compounds were subjected to in vitro cytotoxic screening against breast carcinoma and colon carcinoma cell lines. On the other hand, the antimicrobial activity evaluation of some newly prepared compounds was performed using cup plate diffusion method. Results: It was observed that the oxadiazo...
Research on Chemical Intermediates, 2013
Some novel triazolo[1,5-a]pyridine (4-6), thiazolo[3,2-a]pyridine (7), thiazolo[3,2-a]pyrimidines (9, 11), oxoimidazo[1,2-a]pyrimidine (10), and pyrimido[2,1-b]quinazoline (12) have been synthesized. The structures of target compounds were confirmed by elemental analyses and spectral data. The antimicrobial activity of some of the target synthesized compounds were tested against various microorganisms such as Salmonella typhimurium, Pseudomonas aeruginos and Staphylococcus aureus (bacteria), Aspergillus flavus (fungus), and Candida albicans (yeast fungus) by the disc diffusion method. In general, the novel synthesized compounds showed a good antimicrobial activity against these microorganisms.
Synthesis and Evaluation of Antimicrobial Activity of Pyrimidine Derivatives
Asian Journal of Pharmaceutical and Clinical Research, 2019
Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring. Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro. Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were c...
Synthesis and antimicrobial evaluation of some new pyrimidines and condensed pyrimidines
2013
The reaction of 4-(4-chlorophenyl)-2-mercapto-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 1 with benzylidenemalononitrile and/or methyl iodide has yielded dihydropyrimido[1,2a]pyrimidine derivative 5 and methylthio derivative 6 respectively. Thiated product 7 was cyclized with chloroacetonitrile to give thienopyrimidine derivative 9. Compound 6 was reacted with hydrazine hydrate to give diaminopyrimidine derivative 10. Reaction of 10 with different reagents afforded tetrazolopyrimidine, triazolopyrimidine and pyrimidotriazepine derivatives 11-22. The antimicrobial activity was studied against examples of Gram-positive and Gram-negative bacteria using Tetracycline (Antibacterial agent) and Amphotericin B (Antifungal agent) as standard.
Synthesis of Substituted Pyrimidine Derivatives and Evaluation of their Antimicrobial Activity
2012
Keto group of cyano pyridine moiety have been treated with various aromatic aldehydes to give corresponding chalcones. The Chalcones have been reacted with urea and thiourea to get corresponding novel oxopyrimidines and thiopyrimidines, the structure of all newly synthesized compounds were confirmed by spectral analysis. The synthesized compounds were evaluated for their antimicrobial activity. All the synthesized pyrimidine compounds have show good to moderate antimicrobial activity.
Synthesis and Antimicrobial Activity of Some Newer Derivative of Pyrimidine
Some New Bioactive heterocyclic compounds were synthesize among them pyrimidine compounds were found to possess important pharmacological and antimicrobial properties. Pyrimidine and to chromenes have structural and biological activities relationship so halogenated chromeno pyrimidine were synthesis where structure were characterized by NMR, IR, UB,GC-MS and elemental analysis. They were screened for antimicrobial activity. The Fluoro and methyl Heterocyclic showed highest biological activity.
Recent Advances in Antimicrobial Activity of Pyrimidines: A Review
Asian Journal of Pharmaceutical and Clinical Research, 2021
Over the past era, development of small heterocycles as potential therapeutics has been a zone of major interest. A large number of pyrimidine derivatives are of considerable biological and chemical interest. Pyrimidine derivatives have shown numerous biological activities such as antimicrobial, antitubercular, anticancer, anticonvulsant, antidiabetic, antiviral, and anti-inflammatory. Being a heterocyclic compound, Pyrimidine finds its use for designing synthesis of newer biologically active structures, as its aromaticity makes it relatively stable, also reactive sites which allow for functionalization. Several amino derivatives of nitrogen-containing heterocycles such as pyrimidine, pyridine possess an antimicrobial activity. In this review, recent advancements in the antimicrobial activity of pyrimidine derivatives have been reported.