Antibiotic resistance is the major growing threat facing the pharmacological treatment of bacterial infections. Therefore, bioprospecting the medicinal plants could provide potential sources for antimicrobial agents. Mimusops, the biggest and widely distributed plant genus of family Sapotaceae, is used in traditional medicines due to its promising pharmacological activities. This study was conducted to elucidate the antimicrobial effect of three unexplored Mimusops spp. (M. kummel, M. laurifolia and M. zeyheri). Furthermore, the mechanisms underlying such antibacterial activity were studied. The Mimusops leaf extracts revealed significant antibacterial activities against the five tested bacterial strains with a maximum inhibition zone diameter of 22.0 mm against B. subtilis compared with standard antibiotic ciprofloxacin. The minimal inhibitory and bactericidal concentration values against tested Gram-positive and Gram-negative bacterial strains ranged from 3.15-12.5 µg/ml. However, weak antifungal effect was recorded against Candida albicans with MIC value ˃25 µg/ml. The 1, 1-diphenyl-2-picrylhydrazyl (DPPH) assay showed that M. caffra was the best antioxidant (IC50=14.75±0.028 µg/ml), while M. laurifolia was the least one (IC50=34.22±0.014 µg/ml). The phenolics in plant leaves extracts were identified and quantified by high performance liquid chromatography (HPLC) which revealed the presence of seven phenolic acids and four flavonoids. The abundant phenolic compounds were rutin (5.216±0.067 mg/g dried wt.) and gallic acid (0.296±0.068 mg/g) followed by myricetin (0.317±0.091 mg/g) then kaempferol (0.113±0.049 mg/g) as flavonoids. The antibacterial mechanism of M. laurifolia extract, as a representative species, induces ultrastructural changes in the model bacterium Staphylococcus aureus with cell wall and plasma membrane lysis as revealed by transmission electron microscopy. Overall, Mimusops species (M. laurifolia, M. kummel and M. zeyheri) are promising natural alternative sources for antimicrobial agents.
A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Fina
... Show MoreThis study outlines the synthesis of substituted 1,2,4-triazole derivatives through the cyclization reaction of thiourea derivatives. The process begins with the reaction of different halides with KSCN to produce isothiocyanate derivatives. then followed by a reaction with isonicotinic acid hydrazide to yield thioureas (1-6), with a yield rate of (72-88%). Then, compounds (1-6) were treated with alkaline medium 4 N (NaOH) to produced 1,2,4-triazole derivatives (7-12) with a yield (51-69%).The structure of the prepared compounds was characterized using FTIR,1HNMR and 13CNMR spectroscopy. Some of the synthesized compounds were tested for antimicrobial activity when, compound 9 showed strong activity against gram positive bacteria (Sta
... Show MoreIt is known that the oral administration of ibuprofen caused an irritation of stomach as a side effect due to its carboxylic moiety. Ibuprofen ester was synthesized by linking the carboxylic moiety of ibuprofen and the hydroxylic group of paracetamol to reduce its side effect. Study the kinetic hydrolysis of prepared ester was examined at different values of physiological pH (1.0, 5.8, 6.4 and 7.4) at 37 ± 0.1 of 1 hour period. Measurements of absorbance were carried out by UV-Visible spectrophotometer to follow the stability of ester, it showed Pseudo first order hydrolysis. The pH- apparent rate profiles of ester was exhibited a good stability at pH 1.0 and pH 5.8. Pharmacological activity in vivo of prepared ester was evaluated in re
... Show MoreBackground: Chemotherapeutic medication treatment for cancer is typically used in conjunction with other techniques as part of a routine regimen. It is well established that the capacity of different chemotherapeutic drugs to induce apoptosis is correlated with their anticancer efficacy. Quinazolinone-based drugs have demonstrated excellent responses from several cancer cell types. These substances have a lot of potential for use as building blocks in the creation of apoptosis inducers. Objective: To assess the new quinazolinone derivatives (M1 and M2) that were recently synthesized for their potential to halt wound healing and to use the acridine orange/propidium iodide (AO/PI) double stain to assess their capacity to induce apopto
... Show MoreThe present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia
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