Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Lavanya, G., once mentioned the application of 24242-20-4, Name is 5-Aminopicolinic acid, molecular formula is C6H6N2O2, molecular weight is 138.12, MDL number is MFCD02684600, category is pyridine-derivatives. Now introduce a scientific discovery about this category, Safety of 5-Aminopicolinic acid.
Design, synthesis, spectral characterization and molecular docking studies of novel pyranoquinolinyl dihydropyridine carboxylates as potential antibacterial agents including Vibrio cholerae with minimal cytotoxity towards fibroblast cell line (L-929)
Novel pyranoquinolinyl dihydropyridine carboxylate (PDC) derivatives were designed by incorporating the multi-drug resistance modulating effects of 1,4 dihydropyridines along with potential antibacterial activity of quinolines in the molecular design. The designed PDC derivatives were synthesized by multi-step synthesis involving Michael addition, reduction followed by inverse electro demand Diels-Alder reaction to produce pyranoquinolinyl dihydropyridine carboxylates in good yields. All the PDC derivatives were characterized by H-1 NMR, C-13 NMR, FT-IR, Mass spectral and CHN analysis. The Quinolinyl dihydropyridine carboxylate derivatives were evaluated for in vitro antibacterial activity by agar well diffusion method. Molecular docking studies revealed that the exo diethyl 4-(4aR,58,10bR)-5-(4-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano [3,2-c] quinolin-8-yl) 2,6 dimethyl-1,4-dihydropyridine-3,5-dicarboxylate diastereomer (5c) forms four hydrogen bonds with the cell wall protein of vibrio cholerae in comparison to the endo diethyl 4-((4aR,5R,10bR) 5 (4 chloropheny1)-3,4,4a,5,6,10b-hexahydro-2H-pyrano [3,2-c] quinolin-8-yl)-2,6-dimethyl-1, 4-dihydro pyridine-3,5- dicarboxylate diastereomer (4c) which forms two hydrogen bonds with the cell wall protein of vibrio cholerae and hence leading to better anchorage, enhanced gold score and relatively good antibacterial activity for the exo PDC derivatives. Minimum inhibitory concentration (MIC) of the active compounds was evaluated by macro dilution method. The mechanism of antibacterial action of the PDC derivatives was investigated by SEM studies. The cytotoxicity of PDC derivatives were evaluated against fibroblast cells (L-929).
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem