Biological Evaluation of Compounds with -NCS- Group or Derived from Thiazole and Imidazole. Activity on Prostaglandin Synthetase Complex

Author:

Moulard ThéRése1,Lagorce Jean F1,Thomes Jean C1,Raby Claude1

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, 87025 Limoges Cedex, France

Abstract

Abstract The effects of compounds with activity against thyroid peroxidase were tested on the activity of hydroperoxidase and cyclo-oxygenase of the prostaglandin synthetase complex in-vitro. Active compounds were found to inhibit the peroxidase, and the cyclo-oxygenase function. These compounds were also found to have anti-inflammatory activity as demonstrated by the reduction of carrageenan-induced oedema of the hind paw of the rat. Indomethacin and non-steroidal anti-inflammatory drugs tested under the same conditions were shown to have activity towards the cyclo-oxygenase rather than the peroxidase function of the prostaglandin synthetase complex. A common feature of the active compounds was the presence of an -NCS- linkage or free -SH group.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Reference11 articles.

1. Preferential inhibition of thyroxine and 3,5,3′ triiodothyronine formation by PTU and MMI in thyroid peroxidase catalysed iodination of thyroglobulin;Engler;Endocrinology,1982

2. Mechanism of inactivation of thyroid peroxidase by thioureylene drugs;Engler;Biochem. Pharmacol.,1982

3. Drugs derived from thiazole and imidazole or with nitrogen-carbon-sulfur or tertiary amino groups;Jambut-Absil;Arzneim. Forsch.,1987

4. Formation of molecular iodine during oxidation of iodide;Lagorce;Biochem. Pharmacol.,1991

5. Quantitative study of hydroperoxide reduction by prostaglandin H synthase;Markey;J. Biol. Chem.,1987

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