135764-08-8Relevant academic research and scientific papers
Synthesis and characterization of the novel pyrimidine’s derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity
Abd-Elaziz, Arwa M.,Aly, Hala M.,Fouad, Sawsan A.,Fouda, Amr,Ismail, Abla A.,Saleh, Nashwa M.
, (2021/11/22)
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.
Synthesis of some new 2-(pyrazol-1-yl)-4-(pyrimidin-5-yl)thiazoles
Ahluwalia, V. K.,Sharma, Pooja,Goyal, Bindu,Aggarwal, Renu
, p. 920 - 922 (2007/10/03)
The reaction of 1,3-diaryl-5-chloroacetyl-4,6-dioxo-2-thioxohexahydropyrimidines 2a-h with thiosemicarbazide gives 2-hydrazino-4-[1,3-diaryl-4,6-dioxo-2-thioxohexahydropyrimidin-5-yl]thiazoles 3a-h, which on condensation with acetylacetone yield 4-[1,3-di
SYNTHESIS OF 1,3-DIARYL-1,3-DIHYDRO-4,5-DIOXO-2-THIOXOFUROPYRIMIDINES AND 1,3-DIARYL-1,3-DIHYDRO-2-THIOXO-5(THIAZOL-4-YL)-2H,5H-PYRIMIDINE-4,6-DIONES
Ahluwalia, Vinod Kumar,Sharma, Rashmi,Khanduri, Chandra Has,Kaur, M.,Gupta, Charu
, p. 907 - 914 (2007/10/02)
The reaction of thiobarbituric acids with chloroacetyl chloride in presence of triethylamine afforded 5-chloroacetyl derivatives which on cyclisation with ethanolic sodium acetate gave the corresponding furopyrimidines.Further the 5-chloroacetyl de
Synthesis of 1,3-diaryl-1,3-dihydro-5-(thiazol-4-yl)-2-thioxo-2H,5H-pyrimidine-4,6-diones
Ahluwalia, V K,Chauhan, Anuja,Khurana, Anju,Arora, K K
, p. 1062 - 1064 (2007/10/02)
5-(2-Amino/mercapto-thiazol-4-yl)-1,3-diaryl-1,3-dihydro-2-thioxo-2H,5H-pyrimidine-4,6-diones (3 and 4) have been synthesised and screened for their antifungal and antibacterial activities.
