Collect. Czech. Chem. Commun. 2000, 65, 1082-1092

Synthesis and Biological Evaluation of New Antiinflammatory 1-Benzothiophene-2-carboxanilides

Jiří Svobodaa,*, Michal Štádlera, Antonín Janderab, Vladimíra Panajotováb and Miroslav Kuchařb

a Department of Organic Chemistry, Prague Institute of Chemical Technology, 166 28 Prague 6, Czech Republic
b Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3, Czech Republic


3-Substituted 1-benzothiophene-2-carboxanilides 2-5 and their corresponding sulfones 6-8 were synthesized. The antiinflammatory effect of compounds 2-8 was evaluated in tests of LTB4 biosynthesis, carrageenin edema and ear inflammation. With the exception of 3-hydroxyamides 5a-5c, low inhibitory activities against COX and LT biosynthesis were observed.

Keywords: Benzothiophenes; Sulfones; Antiinflammatory activity; 5-LO inhibition; Calculated log P values.

References: 21 live references.