391-23-1Relevant articles and documents
Design, Synthesis, and Biological and In Silico Study of Fluorine-Containing Quinoline Hybrid Thiosemicarbazide Analogues
Patel, Dhaval B.,Patel, Kinjal D.,Prajapati, Neelam P.,Patel, Krupa R.,Rajani, Dhanji P.,Rajani, Smita D.,Shah, Naumita S.,Zala, Devendra D.,Patel, Hitesh D.
, p. 2235 - 2252 (2019/08/12)
A novel series of fluorine-containing quinoline hybrid thiosemicarbazide analogues (8a–8l) were synthesized and tested for their biological activities. The antibacterial results demonstrated that compounds 8d and 8l [minimal inhibitory concentration (MIC) 62.5?μg/mL] were shown to have higher biological activity than ampicillin against Escherichia coli. Compound 8b (MIC 25?μg/mL) was shown to have the highest activity than was ampicillin against Staphylococcus aureus. The antifungal results demonstrated that compound 8j (MIC 100?μg/mL) has shown good activity. Most of the targeted compounds have shown potent antimalarial activity. Compounds 8d (0.19?μg/mL), 8g (0.30?μg/mL), 8h (0.36?μg/mL), 8k (0.10?μg/mL), 8l (0.28?μg/mL), 8k (0.10?μg/mL), and 8l (0.28?μg/mL) have notable activity than does the reference drug quinine. Compounds 8d (0.27?μg/mL), 8g (0.30?μg/mL), and 8k (0.17?μg/mL) have shown excellent activity against chloroquine-resistant strain. The MTT assay performed on peripheral blood lymphocyte cultures showed a high percentage of lymphocyte viability [8d (99.64), 8g (99.46), 8h (98.83), and 8k (99.51)] at a maximum dose (10?μg/mL), depicting no cytotoxicity of these compounds on human lymphocytes in vitro. A molecular docking study was performed on Pf-DHFR-TS inhibitor. A molecular dynamics study has shown compound 8g to have better affinity with protein. ADME-Tox and pharmacophore study of synthesized compounds suggested prediction of active site.
