Acta Med. 2003, 46: 147-151

Inhibition of Aromatic Amino Acid Decarboxylase by a Group of New Potential Nonsteroidal Anti-Inflammatory Drugs with Antileukotrienic Effects

Jaroslav Dršataa, Miroslav Kuchařb

aCharles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Biochemical Sciences and Research Centre LN00B1251, Hradec Králové, Czech Republic
bZentiva-VÚFB, Prague, Czech Republic

Received June 1, 2003
Accepted October 1, 2003

Possible in vitro inhibition of aromatic amino acid decarboxylase (AAD, EC by a group of phenylsulfonylbenzoic acid derivatives VÚFB 19363, 19369, 19370, 19371, and 19760 as new potential anti-inflammatory compounds was studied using the substrate L-tyrosine. Enzyme inhibition by 2.7x10–5 M concentration of compound VÚFB 19363 (Quinlukast) was 17 %, AAD inhibition at 3.75 x 10–5 M concentration of compounds VÚFB 19369, 19370, 19371, and 19760 ranged between 9–23 %. There were distinct differences between individual compounds. Evaluation of inhibition kinetics suggested full reversibility with VÚFB 19369 and the uncompetitive type of inhibition in the case of compound VÚFB 19363. Considering the anti-inflammatory activity of the compounds studied, the weak AAD inhibition found is rather favourable for their prospective pharmacological effect.


This work was supported by Research project LN00B125 of the Czech Ministry of Education.


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