Synthesis and Evaluation of Antimicrobial Activity of Pyrimidine Derivatives (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.
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 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.
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.
Synthesis, characterization and biological evaluation of substituted pyrimidines
International journal of pharmaceutical research and application, 2021
A series of substituted pyrimidines (SW-1A - SW-5A and SW-1B - SW-5B) synthesized from corresponding chalcones. Chalcones were prepared by Claisen schmidt condensation between p-chloroacetophenone and substituted benzaldehyde and chalcones were then cyclised with guanidine nitrate via Michael’s addition to get substituted pyrimidines. Later the pyrimidines were acetylated and chloroacetylated to yield substituted pyrimidine derivatives. The chemical structures of synthesized compounds were confirmed by IR, NMR spectral studies and the synthesized compounds were screened for antibacterial and antifungal activities by cup-plate method.
ChemInform, 2013
A series of pyrido[2,3-d]pyrimidine derivatives viz 4-amino-5,7-disubstituted pyrido[2,3-d]pyrimidines 3a-d, 4-amino-5,7disubstituted pyrido[2,3-d]pyrimidin-2(1H)-ones 4a-d and 4amino-5,7-disubstituted pyrido[2,3-d]pyrimidin-2(1H)-thione 5ad have been synthesized by the condensation reaction of 2-amino-3-cyano-4,6-disubstituted pyridines 2a-d with formamide, urea and thiourea, respectively. The newly synthesized compounds have been established by elemental analysis, IR, 1 H and 13 C NMR. All the synthesized compounds have been screened for their antibacterial and antifungal 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.
In vitro pharmacological screening of three newly synthesised pyrimidine derivatives
Natural Product Research, 2014
The antibacterial and antifungal activities of three new pyrimidine derivatives, namely, 2,6-bis(4,6-dimethylpyrimidin-2-ylthio)benzene-1,4-diol (1),3,5-bis(4,6-dimethylpyrimidin-2-ylthio)-2-methylbenzene-1,4-diol (2) and 3,5-bis(4,6-dimethylpyrimidin-2ylthio)-2-methoxybenzene-1,4-diol (3), synthesised by electrochemical method are presented here. The compounds were screened for their activities against Grampositive and Gram-negative bacteria, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and a pathogenic fungus Aspergillus niger. The results show that these compounds have significant activity against these bacteria and fungus. The minimum inhibitory concentration of compound 1 was determined as 62.5 mg/mL against B. subtilis, 125 mg/mL against E. coli and 250 mg/mL against S. aureus establishing its promising activities higher than susceptible ranges.
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.