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New Bicyclic Amines: Synthesis and SARs of their Action Against the Causative Organisms of Malaria and Sleeping Sickness

[ Vol. 16 , Issue. 11 ]

Author(s):

R. Weis and W. Seebacher   Pages 1426 - 1441 ( 16 )

Abstract:


Diaryl-substituted bicyclic amines are a scarcely investigated class of compounds. Only few of them are described and their biological activities are reported poorly. During our work in the field of heterocyclic chemistry, we found that 4-dialkylaminobicyclo[2.2.2]octan-2-ones and – ols show antiprotozoal properties against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense, the causative organisms of Malaria tropica and of Human African Trypanosomiasis. Therefore, we synthesized over 200 derivatives in order to investigate their antitrypanosomal and antiplasmodial activities as well as their cyctotoxicity using in vitro microplate assays. Even if the target and the mechanism of action of these compounds are still unknown, we can at least provide several structure-activity relationships for this interesting class of compounds. Moreover, we achieved a distinct improvement of their antiplasmodial and antitrypanosomal properties.

Keywords:

Bicyclic amines, antiplasmodial activity, antitrypanosomal activity, in vitro microplate assays, in vivo assays, structure-activity relationships

Affiliation:

Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitatsplatz 1, A-8010 Graz, Austria.



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