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Braz. J. Pharm. Sci. (Online) ; 56: e18092, 2020. tab, graf
Article in English | LILACS | ID: biblio-1142491


We synthesized a series of compounds bearing pharmacologically important 1,3,4-oxadiazole and piperidine moieties. Spectral data analysis by 1H-NMR, 13C-NMR, IR and EI-MS was used to elucidate the structures of the synthesized molecules. Docking studies explained the different types of interaction of the compounds with amino acids, while bovine serum albumin (BSA) binding interactions showed their pharmacological effectiveness. Antibacterial screening of these compounds demonstrated moderate to strong activity against Salmonella typhi and Bacillus subtilis but only weak to moderate activity against the other three bacterial strains tested. Seven compounds were the most active members as acetyl cholinesterase inhibitors. All the compounds presented displayed strong inhibitory activity against urease. Compounds 7l, 7m, 7n, 7o, 7p, 7r, 7u, 7v, 7x and 7v were highly active, with respective IC50 values of 2.14±0.003, 0.63±0.001, 2.17±0.006, 1.13±0.003, 1.21±0.005, 6.28±0.003, 2.39±0.005, 2.15±0.002, 2.26±0.003 and 2.14±0.002 µM, compared to thiourea, used as the reference standard (IC50 = 21.25±0.15 µM). These new urease inhibitors could replace existing drugs after their evaluation in comprehensive in vivo studies.

Computer Simulation/classification , Salmonella typhi/classification , Sulfonamides/adverse effects , Thiourea , Bacillus subtilis/classification , Urease , Serum Albumin, Bovine , Pharmaceutical Preparations/administration & dosage , Cholinesterase Inhibitors/pharmacology , Inhibitory Concentration 50 , Proton Magnetic Resonance Spectroscopy/methods , Data Analysis , Amino Acids/antagonists & inhibitors