Cancer has emerged as one of the leading causes of deaths globally partly due to the steady rise in anticancer drug resistance. Pyrimidine and pyrimidine-fused heterocycles are some of the privileged scaffolds in medicine, as they possess diverse biological properties. Pyrimidines containing azole nucleus possesses inestimable anticancer potency and has enormous potential to conduct the regulation of cellular pathways for selective anticancer activity. The present review outlines the molecular structure of pyrimidine-fused azoles with significant anticancer activity. The structure activity relationship and molecular docking studies have also been discussed. The current review is the first complete compilation of significant literature on the proposed topic from 2016 to 2020. The information contained in this review offers a useful insight to chemists in the design of new and potent anticancer azole-pyrimidine analogues.
The design of environmentally friendly approach to the synthesis of biologically important compounds without compromising the yield has been the focus of many chemists in recent years. The development of one-pot synthesis of heterocycles in the presence of ionic liquids (ILs), used as both environmental media and catalysts is efficient and environmentally sustainable. This review highlights the one-pot synthesis of imidazoles in acidic ILs in the past decade. Some reviews have been done on imidazoles, such as their pharmacological importance. Hence we decided to focus on their synthesis in acidic ionic liquids, which the authors are not aware of any published literature.
Aims: This study was carried out to evaluate the antibacterial activity of aqueous and ethanol leaf extracts of Ocimum gratissimum and Carica papaya against selected clinical isolates of Gramnegative bacteria and to also determine the phytochemical constituents of the plants. Methodology: Extraction of plant leaves was carried using the cold maceration method and preliminary antimicrobial screening of the extracts was done using the disc diffusion method. The minimum inhibitory concentrations (MICs) of the plant extracts against test organisms were determined using the broth dilution technique. The minimum bactericidal concentrations (MBCs) were also determined. Results: Phytochemical analyses of leaf extracts of both plants revealed the presence of tannins, alkaloids, saponins and anthraquinones. Antibacterial activity was recorded at concentrations ranging from 12.5-50 µg/mL. At 50 µg/mL, the aqueous and ethanol extracts of O. gratissimum showed best activity against E. coli and S. typhi respectively. Also, the aqueous and ethanol extracts of C. papaya recorded good activity against E. coli. The minimum inhibitory concentrations (MICs) of the aqueous extract of C. papaya against test isolates ranged from 12.5-25 µg/mL and
Original Research Articlethat of the ethanol extract ranged from 25-50 µg/mL. O. gratissimum recorded MICs that ranged from 12.5-25 µg/mL for the aqueous extract, and 25 µg/mL for the ethanol extract. The minimum bactericidal concentrations (MBCs) of C. papaya ranged from 25-50 µg/mL for the aqueous extracts and 50 µg/mL for the ethanol extract; and that of O. gratissimum ranged from 12.5-25 µg/mL for the aqueous extract, and 25−50 µg/mL for the ethanol extracts.
Conclusion:This study shows that C. papaya and O. gratissimum leaves have antibacterial activity and supports the traditional use of these plants as medicines.
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