Monu Joy

TL;DR: A series of eleven chlorinated thienyl chalcone derivatives substituted with a different functional groups at the para- position on the ring B investigated for their ability to inhibit human MAO-A and -B and the most potent compound, TC6, was found to be the best activity and higher selectivity towards hMAO-B.

TL;DR: The most potent compound, TB5, showed the best inhibitory activity and higher selectivity toward hMAO‐B, with Ki and SI values of 0.11±0.01 μm and 13.18, respectively.

TL;DR: The most potent MAO-B inhibitor, C5, was found to be nontoxic towards cultured hepatic cells at 5 and 25μM, with 97 and 90% viability, and the most potent compound, (2E)-3-[4-(dimethylamino) phenyl]-1-(4-methoxyphenyl) prop-2-en-1-one (C5), showed the best inhibitory activity towards hMAO- B.

TL;DR: The pharmacophore generation and atom-based three-dimensional quantitative structure-activity relationship (3D-QSAR) analyses of previously reported thiophene-based hMAO-B inhibitors showed good correlation with its predictability of the statistically valid 3D- QSAR analyses.

TL;DR: The interaction between halogenated thiophene chalcones and the main plasma protein, i.e. human serum albumin (HSA), has been investigated in vitro under simulated physiological condition by spectroscopic techniques (UV-Vis, fluorescence and circular dichroism), zeta potential and molecular docking.