Abstract
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.
Keywords: antileukotrienic drugs, aryl bromides, copper catalysts, microplate colorimetric acid phosphatase
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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