Disease relevance of CGP 20376

• Examination of the in vitro effects of CGP 20376 using these viability criteria/assay systems showed some delayed suppression of worm motility, but after 120 h in vitro CGP 20376 was not macrofilaricidal against male or female O. volvulus [1].
• CGP 20376 was fully effective against B.m. and B.p. at 12.5 mg/kg p.o., against L.c. at 25 mg/kg p.o. and against D.v. at 50 mg/kg p.o.. This compound has been selected from this series of novel benzazoles as a first candidate for trials against human bancroftian filariasis [2].

High impact information on CGP 20376

• Thus, CGP 20376 was effective against all life cycle stages of B. malayi in jirds [3].
• Evaluation of suramin, ivermectin and CGP 20376 in a new macrofilaricidal drug screen, Onchocerca ochengi in African cattle [4].
• Three monoclonal antibodies directed towards antigens of Onchocerca gibsoni were used in antigen detection ELISAs to detect parasite antigens in sera from 100 cattle infected with O. gibsoni, in trials with the filaricidal compounds CGP 6140, CGP 20309, CGP 20376, CGP 21833, CGP 24589 and CGP 26702 [5].
• CGP 6140 and CGP 20376 were tested in vivo, using a diffusion chamber technique for the implantation of infective larvae into the peritoneum of Mastomys natalensis and assessing the survival of the implanted parasites [6].

Chemical compound and disease context of CGP 20376

• Electron microscopic examination was used to assess the effects of CGP 6140 (proposed generic name: amocarcine) and CGP 20376 (proposed generic name: metobethiamide) on the fine structure of microfilariae and third stage larvae of Onchocerca volvulus after in vitro exposure to different concentrations of these compounds [7].

Analytical, diagnostic and therapeutic context of CGP 20376

• In the present study, parasite antigen levels were compared to parasitological parameters after treatment of B. malayi-infected jirds with CGP 20376 that has been reported to be active against both microfilariae and adult worms of this parasite [8].
• It was confirmed that the drugs CGP 20376, 21835, 20308, 21306, and 6140 cause a rapid immobilization in vitro of the adult filarial worm, Litomosoides carinii, the time required being similar to rotenone at the same concentration [9].

References