Comparative antifilarial efficacy of the N-oxides of diethylcarbamazine and two of its analogues.
The N-oxides of 1-diethyl carbamoyl-4-methyl piperazine (DEC), 3-ethyl-8-methyl, 1,3,8-triazabicyclo (4,4,0) decan-2-one (centperazine) and 1-methyl-4-(pyrrolidin-1-yl-carbonyl) piperazine (CDRI Comp. 72/70) have been evaluated against Limotosoides carinii infection in cotton rats to establish whether conversion of the three antifilarials into N-oxides would lead to exertion of better antifilarial activity. Of the three N-oxides, N-oxide of DEC showed significantly more suppressive effect on circulating microfilariae in comparison to its parent compound. However, adult worms were unaffected. It was observed that basicity of the N-CH3 group did not play major role in exertion of activity of DEC and related compounds. Nevertheless, two other N-oxides were inactive.
Chatterjee
R K
RK
Parasitology Division, Central Drug Research Institute, Lucknow, India.
Fatma
N
N
Agarwal
V K
VK
Sharma
S
S
Anand
N
N
D000818:Animals; D000871:Anthelmintics / Q000627:therapeutic use*; D004049:Diethylcarbamazine / Q000031:analogs & derivatives / Q000627:therapeutic use*; D005368:Filariasis / Q000188:drug therapy*; D005369:Filaricides / Q000627:therapeutic use*; D005370:Filarioidea / Q000187:drug effects*; D010087:Oxides / Q000627:therapeutic use*; D051381:Rats
D000871:Anthelmintics; D005369:Filaricides; D010087:Oxides; D004049:Diethylcarbamazine