Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 1,5-Diphenylpenta-1,4-dien-3-one, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 538-58-9
gamma-Amino butyric acid analogs as novel potent GABA-AT inhibitors: Molecular docking, synthesis, and biological evaluation
A new series, of gamma-amino butyric acid analogs were designed and synthesized as novel potent GABA-AT inhibitors. A structure-activity relationship study was performed by correlating the effect of different substituents with GABA-AT inhibitory activity of the title compounds. The preliminary bioassays showed that acid hydrazones exhibited excellent inhibitory activities in micromolar (0.07-0.56 muM) range, while Schiff’s bases showed variable results. The most potent compound, 4-amino-N’-[(1Z)-1-(2-bromophenyl) ethylidene]butanehydrazide (AHG177) showed inhibitory potency (IC50) of 0.073 muM. Aminobutyrate transaminase is a pyridoxal-P enzyme which follows a bi-bi ping pong mechanism and in pyridoxamine form can readily transaminate only with succinic semialdehyde and 2-oxoglutarate. The results strongly suggest that only the pyridoxal form of the enzyme is capable of reacting with the ligands. Our findings open up the possibility to extend this protocol to different databases in order to find new potential inhibitor for promising targets based on a rational drug design process.
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Reference£º
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate