391-23-1Relevant academic research and scientific papers
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.
Synthesis and aldose reductase inhibitory activity of N-(quinolinyl thiocarbonyl) glycine derivatives
Nicolaie, E,Guengoer, T,Goyard, J,Cure, G,Fouquet, A,et al.
, p. 977 - 984 (2007/10/02)
The onset of diabetic complications may be prevented by the inhibition of aldose reductase.Derivatives of N-(quinolinyl thiocarbonyl) glycine were prepared and their in vitro and ex vivo aldose reductase inhibitory activities were tested on rat lens.The cincophen derivatives were the most potent in vitro with an enzyme inhibition value of 29percent at 10-8 M and 91percent at 10-7 for the N--N-methylglycine compound 10a.This activity was shown to be dependent on the nature of the substituents and seems to be optimal for the acids; esterswerefound to be inactive.No compound have shown ex vivo inhibitory activity.It is concluded that the lack of ex vivo activity is likely due to a poor bioavailability or a bad penetration of the compounds in target tissue (lens). aldose reductase inhibitors / diabetic complications / N-(quinolinyl thiocarbonyl) glycine
