Copyright © 1999 by Institute of Pharmacology
Polish Academy of Sciences 		Pol. J. Pharmacol., 1999, 51, 257-262
ISSN 1230-6002
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PRELIMINARY COMMUNICATION
 IMMUNOLOGICAL ACTIVITY OF NEW HETEROCYCLIC AMIDES OF 5-AMINO-3-METHYLISOXAZOLE-4-CARBOXYLIC ACID
 Stanis³aw Rynga#, Micha³ Zimeckib, Adam Fedorowiczc, Aleksander Kollc
 a Wroc³aw Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9, PL 50-137 Wroc³aw, Poland,
b Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Department of Experimental Therapy, Weigla 12, PL 53-114 Wroc³aw, Poland,
c University of Wroc³aw, Faculty of Chemistry, F. Joliot-Curie 14, PL 50-383 Wroc³aw, Poland

Immunological activity of new heterocyclic amides of 5-amino-3-methylisoxazole-4-carboxylic acid. S. RYNG, M. ZIMECKI, A. FEDOROWICZ, A. KOLL. Pol. J. Pharmacol., 1999, 51, 257-262.

In the present study, some new amides of 5-amino-3-methylisoxazole-4-carboxylic acid were obtained. All new structures possessed markedly different groups of electron acceptor character, different spatial structure and they contained nitrogen heteroatom, enabling formation of salts and, at the same time, higher biological availability. They were examined for immunomodulating activity in comparison with cyclosporine A (CsA). We investigated effects of the compounds on the lipopolysaccharide (LPS)-induced production of tumor necrosis factor-alfa (TNF-alfa) and interleukin-6 (IL-6) by human peripheral blood cells. Some compounds exhibited suppressory action which corresponded with increasing electronoacceptor nature of the amide substituent. Two compounds, characterized by flat aromatic rings, demonstrated quite different properties. Much higher activity was expressed by compounds which contained -NH group, the group which conditioned immunostimulatory activity in other compounds described previously.

Key words: isoxazoles, immunological activity, amides of isoxazolecarboxylic acid, QSAR, immunostimulator, immunosuppressor
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