Lutz, Toni published the artcileDevelopment of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N-Arylalkynyl Substituents, Name: 4-Chloro-2-methylphenylboronic acid, the publication is ChemMedChem (2017), 12(5), 362-371, database is CAplus and MEDLINE.
A new scaffold of highly potent and mGAT1-selective inhibitors has been developed. Compounds in this class are characterized by an alkyne-type spacer connecting nipecotic acid with an aromatic moiety. Preliminary evaluations made it apparent that a nipecotic acid derivative with an N-butynyl linker and a terminal 2-biphenyl residue exhibiting a binding affinity (pKi) of 7.61±0.03 to mGAT1 and uptake inhibition (pIC50) of 7.00±0.06 selective for mGAT1 could serve as a hit compound Docking calculations for compounds based on this structure in an hGAT1 homol. modeling study indicated binding affinities similar to or even higher than that of the well-known mGAT1 inhibitor tiagabine. Synthesis of the designed compounds was readily carried out by two consecutive cross-coupling reactions, giving flexible access to variously substituted biphenyl subunits. With an appropriate substitution pattern of the biphenyl moiety, the binding affinity of enantiopure (R)-nipecotic acid derivatives to mGAT1 increased to pKi=8.33±0.01, and the uptake inhibitory potency up to pIC50=7.72±0.02.
ChemMedChem published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Name: 4-Chloro-2-methylphenylboronic acid.
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