Study of ADMET Descriptors of Novel Chlorinated N-Arylcinnamamides

Abstract

A series of seven (2E)-3-(3,4-dichlorophenyl)-N-arylprop-2-enamides was prepared. Six compounds from this limited set were mono-and di-chlorinated not only on the aromatic ring of acid but also on the anilide ring. The compounds have been proposed as potential anti-infective, anti-inflammatory, and anti-cancer agents. Since lipophilicity significantly affects the biological activities and the pharmacokinetic profile of compounds, the hydro-lipophilic properties of these new highly chlorinated compounds were experimentally studied. At the same time, the overall ADMET profiles of the compounds were investigated to establish whether they comply with the Lipinski's Rule of Five and thus meet the qualitative concepts of "druglikeness" for new bioactive molecules. All the discussed compounds were analyzed using the reversed-phase high performance liquid chromatography method. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase, using an end-capped non-polar C18 stationary reversed-phase column. In the present study, the structure-lipophilicity relationships of the studied compounds are discussed.