Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transform infrared (FT-IR) spectroscopy, and Proton nuclear magnetic resonance (1H-NMR) spectroscopy were used to establish the purity and characterization of these derivatives. When compared to standard antibiotics (Sulfamethoxazole, Ciprofloxacin, and Fluconazole), the preliminary antimicrobial activity tests on four different bacteria strains and one type of fungus demonstrated that the final compounds (M1-M6) have significant activity. Finally, the new derivatives (M3 and M5) are the most potent than the other ones and more active than the standard drugs.
Five species of Lactic acid bacteriawere isolated from raw milk, yoghurt, vegetables and pickles, Lactobacillus plantarum, Lactobacillus acidophilus, Lactobacillus brevis, Lactobacillus casei and Lactobacillus bulgaricus isolates were identified by 16S rRNA gene. Evaluate of antimicrobial activity against all the bacterial strains Staphylococcus aureus, Salmonella spp., Pseudomonas fluorescens, Escherichia coli, Bacillus cereus and Bacillus subtilis. It showed that bacteriocin of Lactic acid bacteriamore effective than supernatant of lactic acid bacteria, the results showed that isolatemost efficient isolate belonging to Lactobacillus brevis, the diameter of the inhibition of the bacteriocin of Lactobacillus brevis were 27.7, 26.3 and 25.1
... Show Moren this work, a series of new nucleoside analogues (β-glucose liked to pyrazoline moiety) was synthesized. In the beginning, chalcone [1-3] was formed from the reaction of acetophenone and benzaldehyde derivatives in the presence of sodium hydroxide. Pyrazolines [4-6] were obtained from the reaction of the prepared chalcones and hydrazine hydrate in the presence of ethanol absolute. These pyrazolines were treated with β-glucose pentaacetate to afford a series of desirable protected nucleoside analogues [8-10]. After that hydrolysis of protected nuclioside analogues in sodium methoxide gave free nucleoside analogues [11-13]. These new formed compounds were diagnosed by 13C-NMR and 1H- NMR for some of them and FT-IR spectroscopy.
Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1
... Show MoreCampsis grandiflora (Bignoniaceae) is a fast growing deciduous climber, the dried flowers have been used as a carminative, blood tonic, and febrifuge in Chinese traditional medicine. This plant has an anti-inflammatory, anti-oxidant, anti-depressant, and anti-bacterial effect; with a beneficial role in stagnant blood and endometriosis conditions. In this study, the detection of beta-sitosterol in the hexane extract of Iraqi C.grandiflora flowers was performed using thin layer chromatography (TLC) and high performance liquid chromatography(HPLC); while the isolation done by preparative layer chromatography then structure elucidation of isolated compound was done by FTIR and 1HNMR. Furthermore, assessment of th
... Show MoreEtodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects co
... Show MoreZerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5 % at
... Show MoreZerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5
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