title: Comparative antifilarial efficacy of the N-oxides of diethylcarbamazine and two of its analogues.
abstract: 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.
authors.affiliation: Parasitology Division, Central Drug Research Institute, Lucknow, India.
authors.forename: R K
authors.initials: RK
authors.lastname: Chatterjee
authors.forename: N
authors.initials: N
authors.lastname: Fatma
authors.forename: V K
authors.initials: VK
authors.lastname: Agarwal
authors.forename: S
authors.initials: S
authors.lastname: Sharma
authors.forename: N
authors.initials: N
authors.lastname: Anand
mesh_terms: 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
chemical_list: D000871:Anthelmintics; D005369:Filaricides; D010087:Oxides; D004049:Diethylcarbamazine