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Elsevier, European Journal of Medicinal Chemistry, (63), p. 457-467

DOI: 10.1016/j.ejmech.2013.02.019

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Synthesis, biological activity and resistance to proteolytic digestion of new cyclic dermorphin/deltorphin analogues

Journal article published in 2013 by A. Krzysztof Ba�nkowski, D. Zbigniew Szewczuk, Krzysztof Bankowski, B. Ewa Witkowska, Ewa Witkowska, A. Olga M. Michalak, Olga M. Michalak, A. Katarzyna Sidoryk, Katarzyna Sidoryk, A. Ewa Szymanek, Ewa Szymanek, C. Bo_zena Antkowiak, Bożena Antkowiak, C. Ma1gorzata Paluch, Małgorzata Paluch and other authors.
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This paper is available in a repository.

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Abstract

A series of novel cyclic ureidopeptides, analogues of dermorphine/deltorphine tetrapeptide, were synthesized by solid phase peptide synthesis and/or in solution. The antinociceptive activity of N-substituted amides 1-10 was evaluated using hot-plate and tail-flick tests. Analogue 1 showed significant, stronger than morphine, antinociceptive effect after systemic applications. All analogues were also tested for their in vitro resistance to proteolysis by means of mass spectroscopy and it was found that all substituted amides 1-10 showed full stability during incubation with large excess of chymotrypsin and pepsin. Compound 1 is a lead molecule for further evaluation.