Saccharin is firstly synthesized in 1879. It is a very well-known as an inexpensive substitute for sugar as it is a non-caloric sweetener. The article shows the properties, use, metabolism and various synthesis and reactions of saccharine. Moreover, the toxicological reports explain that saccharin is mostly responsible for the bladder tumors observed in the male rats, the relationship between the consumption of saccharin and bladder cancer is afforded by epidemiological studies. The benefit-risk evaluation for saccharin is hardly to indicate. Saccharin is a sugar substitute, frequently used either in food industry, or in pharmaceutical formulations and even in tobacco products. The chemistry of saccharin is interesting because of it suspected carcinogenous character and the possible use as an antidote for metal poisoning. It appears prudent to evaluate their main properties and applications further.
Objective: This study goal was to screen participants from different settings in Baghdad for depression using Beck Depression Inventory (BDI) scale and identify factors influencing the levels of depression. Methods: This cross-sectional study included a convenience sample of 313 people from four settings (teaching hospital, college of medicine, college of pharmacy, and high school) in Baghdad, Iraq. The participants were screened using paper survey relying on the BDI scale during spring 2018. Using multiple linear regression analysis, we measured the association between depression scores and six participant factors. Results: The overall prevalence of depression in our sample was 57.2%. Female participants had higher BDI scores (depression symptoms) than male participants. Among those with depression, the majority (73.7%) had mild or moderate degree of depression. In terms of the cut-off scores, 42.8 % scored in the normal range, 20.4 % in the mild range, 7.0 % in the borderline range, 14.7 % in the moderate range, 10.5 % in the severe range and 4.5 % in the very severe range depression. Approximately 63% of the participants had sort of suicidal thoughts. The regression analysis showed significant (P-value < 0.05) association between having higher scores of depression symptoms and the presence of chronic disease(s), recent family loss, young age and female gender. Conclusions: In our findings, depression was quite prevalent among people in Iraq. The study demonstrates the importance of broad screening and social/psychiatric counseling of young population. Iraqi healthcare professionals should structure specific actions for patients with chronic diseases to minimize their depression symptoms. Article Type: Orignal Research
Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.
Objective: Pyrimidine derivatives are reported to possess antibacterial, antifungal, anticancer, and anticonvulsant activities. Encouraged by this remarks, we decided to synthesize novel compounds of new 2-macraptopyrimidine linked to Schiffs̕ bases. Methods: The present work involves the synthesis of new 2-mercaptopyrimidine linked to Schiffs̕ bases. The starting, 2-mercaptopyrimidine, compound (1) reacted with thiourea to afford the corresponding 1-(pyrimidin-2-yl) thiourea (2). Then compound (2) was used as the key intermediate to prepare the -1-(2-hydroxy benzylidene)-3-(pyrimidin-2-yl) thiourea (3), and (1-benzylidine)-3-(pyrimidin-2-yl) thiourea (4), through the reaction with 2-hydroxybenzaldehyde, and benzaldehyde, respectively. Results: All the synthesized compounds were characterized by Fourier-transform infrared and1H-nuclear magnetic resonance spectroscopy. The synthesized derivatives were screened for their in vitro, antibacterial activity against two Gram-positive bacteria: Bacillus subtilis and Staphylococcus aureus and four Gram-negative bacteria: Klebsiella pneumoniae, Escherichia coli, and Salmonella typhi, and the results showed that most of them have good antibacterial activity. While their antifungal activity against three fungi species (Aspergillus fumigates, Aspergillus niger, Aspergillus terrus and Rhizopus) revealed that compounds (2-4) displayed the most potent antifungal activity. Density functional theory (DFT) calculations for the synthesized 2-mercapto pyrimidine derivatives were conducted, using a molecular structure with optimized geometry. Highest occupied molecular orbital/lowest unoccupied molecular orbital energies and structures are demonstrated. Conclusion: The antimicrobial activity indicates that compounds (3) and (4) are the most active than the compounds (1) and (2). Molecular docking revealed that compounds (3) and (4), with bulky phenyl groups are essential to blocking the active centers of glucose -6-phosphate synthase in the bacteria and fungi.
Dihydropyrimidinone and dihydropyrimidine derivatives are reported to possess broad biological activities. Many synthetic samples have been studied as antibacterial, antiviral, and anticancer agents. We decided to synthesize novel compounds of new pyrimidine derivatives. The present work involves the synthesis of new dihydropyridine derivatives. The starting vanillin, compound (1) was used as the key intermediate to prepare the 5-acetyl-4-(4-hydroxy-3-methoxyphenyl)-6-methyl pyrimidine-2(1H)-one(2),Ethyl 4-(4-hydroxy-3-methoxyphenyl)-6-methyl-2-oxo-1,2-dihydropyrimidine-5-carboxylate (3), 4-(4-hydroxy-3-methoxyphenyl)-5,6,7,8-tetrahydro quinazoline-2(1H)-one (4), respectively, through the reaction with urea and acetylacetone or ethyl acetoacetate or cyclohexanone but 4-(4-hydroxy-3-methoxyphenyl)-5,6,7,8-tetrahydro quinazoline-2(1H)-thione (5) reacted with thiourea and cyclohexanone. FTIR,1H-NMRand13C-NMR spectroscopy characterized all the synthesized compounds. The synthesized derivatives were screened for their in vitro, antibacterial activity against two gram-positive bacteria: Bacillus subtilis, and Staphylococcus aureus and two gram-negative bacteria: Klebsiella pneumonia and Salmonella typhi and the results showed that most of them have good antibacterial activity. While their antifungal activity against three fungi species: (Aspergillus fumigates, Aspergillus niger, and Rhizopus), revealed that compounds (1-5) displayed the most potent antifungal activity. Density functional theory ( DFT) calculations for the synthesized compounds (1-5) were conducted, using a molecular structure with optimized geometry. Highest occupied molecular orbital/lowest unoccupied molecular orbital energies and structures are demonstrated. The antimicrobial activity indicates that compounds 3 and 4 are the most active than the compounds 2 and 5. Molecular docking revealed that compounds (4) and (5), with cyclohexyl groups are important to block the active centers of glucose -6-phosphate synthase in the bacteria and fungi.
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