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NEW AMINOCARBONYL DERIVATIVES OF 1-ARYLIMIDAZOLIDINE-2 WITH POTENTIAL PHARMACOLOGICAL ACTIVITY.

Marzena Rządkowska 1Elżbieta Szacoń 1Dariusz Matosiuk 1Sylwia Fidecka 2Ewa Kędzierska 2

1. Medical University, Faculty of Pharmacy, Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Staszica 6, Lublin 20-081, Poland
2. Department of Phamacology and Pharmacodynamics, Staszica 6, Lublin 20-081, Poland

Abstract

The aminocarbonyl derivatives of 1-aryl-2-imidazolidine-2 both chain or fused were found to have significant antinociceptive activity connected with activation of the MOP (mu opioid protein) receptor [1-3]. Recent results on the chain (imidazol-2-yl)urea derivatives are implementing the pharmacophorie model with new features, which have to be taken under consideration in planning further synthesis.

Series A compounds exhibited significant antinociceptive activity in the "writhing test", reversed by small dose (5mg kg-1 i.p.) of naloxon.

ela_2_1.gif

R = H, 2-CH3, 4-CH3, 2-OCH3, 4-OCH3, 2-Cl, 3-Cl, 4-Cl

n = 1, 2

The structure of all new compounds was confirmed by elemental analysis, as well by the 1H NMR spectra.

[1] D. Matosiuk, S. Fidecka, L. Antkiewicz-Michaluk, I. Dybała, A.E.Kozioł, Eur. J. Med.. Chem. 2001, 36, 783.

[2] D. Matosiuk, S. Fidecka, L. Antkiewicz-Michaluk, J. Lipkowski, I. Dybała, A.E.Kozioł, Eur. J. Med.. Chem. 2002, 37, 761.

[3] K.Sztanke, S. Fidecka, E. Kędzierska, Z. Karczmarzyk, K. Pihlaja, D. Matosiuk, Eur. J. Med.. Chem. 2005, 40, 127.

 

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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Elżbieta Szacoń
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-04-07 10:51
Revised:   2009-06-07 00:44