Synthesis of the oxazolone derivatives was achieved by the condensation of aromatic aldehydes with N-acetyl glycine in the presence of acetic anhydride and anhydrous sodium acetate. A total of six oxazolones were 1 13 synthesized and characterized using H-NMR, C-NMR and FT-IR spectroscopic techniques. The synthesized compounds were screened for their in vitro antibacterial and antifungal activities using streptomycin and ampicillin as control. The result showed that some of the compounds demonstrate good antibacterial activities against specific bacterial strains and moderate activities against other bacterial strains. The compounds did not show any sensitivity against the tested fungal strains. The quantitative structure-antibacterial activity relationship was studied using some quantum chemical parameters with the aid of Spartan 10 (V1.0.1) and XLSTAT (add-in) software. A good correlation was observed between the antibacterial activity of the compounds and the calculated quantum chemical descriptors.
Introduction: The history of the relationship between man and plants is as old as creation and man has used plants for different purposes including food and medicines. In this dispensation, man has been able to classify plants into food and medicinal plants and has also discovered that solution to his health problem comes from nature. Objectives: The antibacterial activities of the dichloromethane (DCM) and aqueous (AQU) fractions of acetone extract of Dacryodes edulis leaf were investigated against both Gram positive and Gram negative bacterial organisms made up of locally isolated and standard strains. Materials and Methods: About 1 kg of the powdered leaves of D. edulis was extracted at room temperature (25-27oC) using 75% acetone for 3 days. The mixture was then filtered and the filtrate was dried in vacuo using a rotary evaporator (insert the make and model). The crude extract was successfully partitioned using organic solvents in order of their polarity, that is, n-Hexane, DCM, n-Butanol, Ethylacetate. The sensitivity testing of the extracts against the organisms was determined using agar-well diffusion method as described by Irobi et al. [1]. Results: DCM and aqueous (AQU) fractions possessed closely related broad spectrum antibacterial activities and greater activity than the control standard antibiotics (Streptomycin and Ampicillin). The zones of inhibition exhibited by AQU fraction ranged between 20 and 30 mm while that of DCM fraction ranged between 22 and 32 mm. On the other hand, the zones of inhibition observed for the standard antibiotics, streptomycin ranged between 10 and 20 mm and ampicillin between 11 and 27 mm. The MIC and MBC of both fractions had range values between 0.78 and 6.25 mg/mL, evaluation of phytochemical composition of D. edulis revealed alkaloid (30.63 mg/g), terpenoid (19.72 mg/g), saponins (10.54 mg/g), tannin (9.14 mg/g), flavonoid (6.51 mg/g) and glycoside (6.29 mg/g) which are very significant antibacterial agents in medicinal plants. Conclusion: This work indicates that the two fractions had better antibacterial potentials than the standard antibiotics used.
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