Preparation of 2-(4-{[4-(Quinolin-2-ylmethoxy)phenyl]sulfanyl}phenyl) Propionic Acid (VUFB 20615) and 2-Methyl-2-(4-{[4-(quinolin-2- ylmethoxy)Phenyl]sulfanyl}phenyl)Propionic Acid (VUFB 20623) as Potential Antileukotrienic Agents

The synthesis of racemic 2-(4-{[4-(quinolin-2-ylmethoxy)phenyl]sulfanyl} phenyl)propionic acid (VUFB 20615) and preparation of 2-methyl-2-(4-{[4-(quinolin-2-ylmethoxy)phenyl]sulfanyl}phenyl)propionic acid (VUFB 20623) as new potential antileukotrienic drugs are described. Due to a low reactivity of the 4-substituted aryl bromides (coupling of the 4-substituted aryl bromides do not provide an activating functional group with 4- methoxybenzene-1-thiol), special conditions, in particular specific heterogeneous copper catalysts, were used. Various methods of 2-substituted propionic acid preparation have been discussed in the paper. In vitro cytotoxicity testing was performed using a microplate colorimetric acid phosphatase assay. Antiplatelet activity was evaluated using in vitro test in human platelet-rich plasma.