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Synthesis and characterization of the novel pyrimidine's derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity.
- Source :
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Journal of the Iranian Chemical Society . Jun2022, Vol. 19 Issue 6, p2279-2296. 18p. - Publication Year :
- 2022
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Abstract
- Herein, the biological activities including antibacterial, antifungal, and in-vitro cytotoxicity for some novel substituted pyrazolo[3,4-d]pyrimidinone, benzylidene dihydropyrimidine, pyrano[2,3-d]pyrimidine, hexahydropyrimido[4, 5-d]pyrimidinone, tetrahydropyrido[2,3-d]pyrimidine-6-carbonitrile, and pyrido[2, 3-d:6,5-d'] dipyrimidinone derivatives were investigated. The synthesized novel compounds were achieved through the incorporation of the active moieties such as halo compound, pyrazolo, pyrano, pyrimido, pyrido-derivatives with active methylene group in thiobarbituric acid derivatives at C-5. Structures of all synthesized compounds were characterized by spectral techniques including IR, 1H-NMR, MS, and 13C-NMR. All synthesized compounds were screened for their antibacterial and antifungal activity, while the most promising compounds were selected to investigate their in-vitro cytotoxic efficacy against normal Vero cells and cancerous Caco-2 cells. Data showed that the biological activities were concentration-dependent. All novel pyrimidine derivatives exhibited broad-spectrum antimicrobial activity with a varied zone of inhibition ranging between 11.3 ± 0.6 and 25.3 ± 0.6 mm. The MIC values are different according to a pathogenic organism (ranging between 3.91 and 500 µg mL−1), whereas the MBC/MFC were 2 × to 4 × MIC value. Data of in-vitro cytotoxicity confirm the efficiency of selected novel pyrimidine derivatives to target Caco-2 cancerous cells at low concentrations more Vero normal cells. Four selected compounds 4, 7b, 10, and 12 displayed IC50 values of 286.73 ± 4.54, 138.07 ± 8.21, 332.48 ± 18.75, and 241.18 ± 15.60 µg mL−1, respectively, for normal Vero cell line, whereas it was 271.55 ± 3.68, 65.94 ± 2.36, 121.16 ± 4.96, and 82.28 ± 4.08 µg mL−1, respectively, for Caco-2 cancerous cell line. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 1735207X
- Volume :
- 19
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- Journal of the Iranian Chemical Society
- Publication Type :
- Academic Journal
- Accession number :
- 156743696
- Full Text :
- https://doi.org/10.1007/s13738-021-02448-w