Activity of N,N-dimethy-1-2-propen-1-amine derivatives in mice experimentally infected with Trypanosoma cruzi.
Propenamine derivatives 3-(4'-bromo-[1,1'-biphenyl]-4-yl)-3-(4-X-phenyl)-N,N-dimethyl-2-prope n-1-amine (where X = H or Br) were tested in experimentally infected mice with Trypanosoma cruzi (Y strain). When a daily dose of 20 mg kg-1 of the bromo (X = Br) derivative for 9 consecutive days was used, no parasite by optical microscopy was found. Significant parasitemic decrease was also observed with a single dose (100 mg kg-1) of this compound. Moreover, both treatment schemes displayed a strong protective effect characterized by decreased of mortality. On the other hand, similar treatment schedules using the unsubstituted (X = H) derivative led to parasitemic and mortality curves similar to the control group. These results indicate that the bromo derivative has a remarkable activity against T. cruzi infection. Due to the potentiality of this derivative, further investigation of this class of compounds as chemotherapeutic agents for Chagas' disease is of prime importance.
Pereira
D G
DG
Instituto de Química, Universidade Estadual de Campinas, São Paulo, Brazil.
de Castro
S L
SL
Durán
N
N
D000499:Allylamine / Q000031:analogs & derivatives* / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D001713:Biphenyl Compounds / Q000627:therapeutic use* / Q000633:toxicity; D014355:Chagas Disease / Q000188:drug therapy*; D008297:Male; D051379:Mice; D018512:Parasitemia / Q000188:drug therapy*; D014344:Trypanocidal Agents / Q000627:therapeutic use* / Q000633:toxicity
C113995:3-(4'-bromo-(1,1'-biphenyl)-4-yl)-3-(4-phenyl)-N,N-dimethyl-2-propen-1-amine; C113996:3-(4'-bromo-(1,1'-biphenyl)-4-yl)-3--(4-bromophenyl)-N,N-dimethyl-2-propen-1-amine; D001713:Biphenyl Compounds; D014344:Trypanocidal Agents; D000499:Allylamine