Synthesis and characterization of the novel pyrimidine’s derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity

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, 1 H-NMR, MS, and 13 C-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

Light enhanced the antimicrobial, anticancer, and catalytic activities of selenium nanoparticles fabricated by endophytic fungal strain, Penicillium crustosum EP-1

“…This activity can be related to the efficacy of Se-NPs to inhibit the ergosterol pathways that lead to alteration of sterol profile in the cell wall of Candida spp. 57 , 58 . Also, Se-NPs can be highly accumulated in the Candida cell wall by chemisorption, leading to the mixing of the cell wall proteins with selenium and hence destroying the amino acid containing sulfur such as cysteine and methionine 59 .…”

Recent advancements in the multicomponent synthesis of heterocycles integrated with a pyrano[2,3-d]pyrimidine core

“…Successively, Abd-Elaziz et al 29 have conveyed a simple route for the synthesis of hexahydro-2 H -pyrano[2,3- d ]pyrimidines 3. Therefore, three-component one-pot reactions of N , N -diaryl-thiobarbituric acids with benzaldehyde, and malononitrile or ethyl cyanoacetate in ethanol/TEA provided the anticipated pyranopyrimidines 3 in reasonable yields.…”

“…In addition, compound 3b (IC 50 = 138.07 ± 8.21 μg mL −1 ) exhibited potent cytotoxic activity on Caco-2 cancerous cell lines along with the lowest cell viability percentage at the higher sample concentration applying MTT assay. 29 …”

Phyco-Synthesized Zinc Oxide Nanoparticles Using Marine Macroalgae, Ulva fasciata Delile, Characterization, Antibacterial Activity, Photocatalysis, and Tanning Wastewater Treatment

“…After that, the MB dye solution containing the nanocatalyst was incubated either in dark or light at 35 • C and pH 7 under aeration condition. During the experiment, 2 mL of the treatment was withdrawn at regular interval times (20,40,60,80,100,120, and 140 min) and subjected to centrifugation at 5000 rpm for 10 min. The control was running with the experiment under the same conditions (stirring in the presence or absence of light irradiation) in absence of nanocatalyst.…”

“…They are also incorporated into a wide variety of applications such as optoelectronics, optics, the rubber industry, the textile industry, cosmetic and sunscreen products because of their high properties of UV adsorption, solar cells, concrete production, photocatalysis, biological sensing, gene delivery, and larvicidal, antibacterial, and antifungal agents [16][17][18]. Bacterial infections and the increasing antibiotic-resistant microbes are the main challenges, and a development of new bioactive compounds to overcome their negative effects on human and animal health is very important [19,20]. ZnO of nanoscale-size particles has significant effects as an antimicrobial agent against Gram-positive bacteria, Gram-negative bacteria, and uni-and multicellular fungi compared to the microscale-size particles.…”