title: The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes.
abstract: 3-Azabicyclo[3.2.2]nonanes are already reported as antiprotozoal agents. Structural variations were performed by attachment of several basic side chains, being part of drugs in use, to the ring nitrogen. The structures of the new compounds were established using one and two dimensional NMR measurements. All compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K1(multiresistant) and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. The results are compared to the activities of formerly synthesized compounds. Structure-activity relationships are discussed.
authors: Center for Research in Molecular Medicine, The University of Lahore, Lahore, Pakistan.
authors: Sarfraz
authors: S
authors: Ahmad
authors: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstrasse 1, 8010, Graz, Austria. we.seebacher@uni-graz.at.
authors: Werner
authors: http://orcid.org/0000-0002-5673-0470
authors: W
authors: Seebacher
authors: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstrasse 1, 8010, Graz, Austria.
authors: Johanna
authors: J
authors: Faist
authors: Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002, Basel, Switzerland.|University of Basel, Petersplatz 1, 4003, Basel, Switzerland.
authors: Marcel
authors: M
authors: Kaiser
authors: Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002, Basel, Switzerland.|University of Basel, Petersplatz 1, 4003, Basel, Switzerland.
authors: Reto
authors: R
authors: Brun
authors: Institute for Chemistry and Technology of Materials (ICTM), Graz University of Technology, Stremayrgasse 9, 8010, Graz, Austria.
authors: Robert
authors: R
authors: Saf
authors: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstrasse 1, 8010, Graz, Austria.
authors: Robert
authors: R
authors: Weis
mesh_terms: D000473:Alkanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D053961:Azabicyclo Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D021261:Parasitic Sensitivity Tests / Q000379:methods; D010963:Plasmodium falciparum / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects / Q000502:physiology
chemical_list: D000473:Alkanes; D000981:Antiprotozoal Agents; D053961:Azabicyclo Compounds; C017573:nonane
keywords: 3-Azabicyclo[3.2.2]nonanes; Antimalarial activity; Antitrypanosomal activity; Basic side chains; Structure–activity relationships