Synthesis and evaluation of the in vivo trypanocidal activity of water soluble organotin compounds.
A series of (3-(2-methoxy)ethoxypropyl)tin derivatives were synthesized as potential trypanocidal drugs. The series included an alkyltin trichloride, a dialkyltin dichloride and the corresponding dialkyltin oxide, and six dialkyltin dithio derivatives. Compounds were evaluated for trypanocidal activity using in vitro cultures of Trypanosoma equiperdum and mice infected with the same strain of parasite for in vivo tests. Two of the title derivatives, the bis (3-(2-methoxy)ethoxypropyl)tin dichloride 2 and the corresponding bis (3-(2-methoxy)ethoxypropyl)tin oxide 3, appeared to be water soluble reagents. Furthermore, they are the first examples of organotin compounds presenting interesting in vivo trypanocidal activity.
Laboratoire de Chimie Bio-Organique, Université Victor Segalen Bordeaux 2, 146, rue Léo Saignat, 33076 Cedex, Bordeaux, France.
J
J
Susperregui
M
M
Bayle
G
G
Lain
C
C
Giroud
T
T
Baltz
G
G
Déléris
D000818:Animals; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D009947:Organotin Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects; D014352:Trypanosomiasis / Q000097:blood / Q000188:drug therapy / Q000469:parasitology
D009947:Organotin Compounds; D014344:Trypanocidal Agents