Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity.
A novel series of alkyl- or aralkyl-substituted polyamine analogues was synthesized containing a 3-7-3 polyamine backbone. These analogues were evaluated in vitro, and in one case in vivo, for activity as antitrypanosomal agents, and for activity against opportunistic infection caused by Microsporidia. Compound 21 inhibits trypanosomal growth with an IC(50) as low as 31nM, while compound 24 shows promising activity in vitro against trypanosomes, and against Microsporidia in vitro and in vivo.
Zou
Y
Y
Department of Pharmaceutical Sciences, Wayne State University, Detroit, MI 48202, USA.
Wu
Z
Z
Sirisoma
N
N
Woster
P M
PM
Casero
R A
RA
Weiss
L M
LM
Rattendi
D
D
Lane
S
S
Bacchi
C J
CJ
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D009670:Encephalitozoon cuniculi / Q000187:drug effects; D020128:Inhibitory Concentration 50; D051379:Mice; D018345:Mice, Knockout; D016816:Microsporida / Q000187:drug effects; D011073:Polyamines / Q000737:chemistry* / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects
D000981:Antiprotozoal Agents; D011073:Polyamines; D014344:Trypanocidal Agents