Eu,: J. Med. Chem. 33 (1998) 831-836 0 Elsevier, Paris New products Synthesis, immunomodulating effects and sltructure-activity relationships of new N-phenyl-S-amino-3-methyliso:~azole-4-carboxamides ' Stanislaw Rynga*, Zdzislaw Machofi", Zbigniew Wieczorekb, Michal Zimeckib, Maria MokroszC "Department of Organic bDepartment Chemistry, Faculty of Pharmacy, University ofMedicine, 9 Grodzka, SO-137 Wroclaw, Poland of Experimental Therapy, Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 12 Weigla, 53-1'14 Wroclaw, Poland Chemistq Institute of Pharmacology, Polish AcaL!emy of Sciences, 12 Smetna, 31-343 Krakdw, Poland `Department of Medicinal (Received 16 April 1998; accepted 11 May 1998) isoxazoles / N-phenyl-Samino-3-methylisoxazole-4-carboxamides / immunological activity / structure-activity relationships 1. Introduction Immunostimulatory drugs are considered as a useful supplement in the chemotherapy of cancer and diseases related to immunodeficiencies. In 1971 Renoux discovered that anthelmintic drug levamisole was able to increase the immune response [l]. Many synthetic substances, structurally relevant, or not, to levamisole, have been prepared and their immunological profiles investigated [2-91. A new immunomodulating compound used for treatment of autoimmune disorders, named leflunomide I (HWA-486), was synthesized [lO-131 which structurally resembles the compounds studied in this paper. In the course of our studies on the reactivity and the biological properties of the isoxazole derivatives we have found
European Journal of Medicinal Chemistry – Elsevier
Published: Oct 1, 1998
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