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

Author(s): Josef Jampilek, Martin Dolezal, Jiri Kunes, Petra Víchova, Ivan Raich, Daniel Jun, Robert O'Connor, Martin Clynes.

Journal Name: Current Organic Chemistry

Volume 8 , Issue 13 , 2004

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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

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Article Details

VOLUME: 8
ISSUE: 13
Year: 2004
Page: [1235 - 1243]
Pages: 9
DOI: 10.2174/1385272043370041
Price: $58

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