Synthesis and antiplatelet activity of antithrombotic thiourea compounds: biological and structure-activity relationship studies.

ABSTRACT: The incidence of hematological disorders has increased steadily in Western countries despite the advances in drug development. The high expression of the multi-resistance protein 4 in patients with transitory aspirin resistance, points to the importance of finding new molecules, including those that are not affected by these proteins. In this work, we describe the synthesis and biological evaluation of a series of N,N'-disubstituted thioureas derivatives using in vitro and in silico approaches. New designed compounds inhibit the arachidonic acid pathway in human platelets. The most active thioureas (compounds 3d, 3i, 3m and 3p) displayed IC50 values ranging from 29 to 84 µM with direct influence over in vitro PGE2 and TXA2 formation. In silico evaluation of these compounds suggests that di

SUBMITTER: Lourenco AL 

PROVIDER: S-EPMC6272548 | biostudies-literature | 2015 Apr

REPOSITORIES: biostudies-literature