A new agent for the treatment of liver fluke infection (Fascioliasis)

Progress in the Experimental Chemotherapy of Helminth Infections; Part I, Trematode and Cestode Infections

“…To date, structure-activity relationships within the series do not appear to have been published, although the most promising compound 3' -chloro-4' -(p-chlorophenoxy)-3, 5-diiodosalicylanilide (rafoxanide) (LIX) has since been introduced into veterinary medicine [142]. Interestingly, rafoxanide appears to be one of the very few compounds that is active against F. hepatica, Schistosoma mansoni and Hymenolepis species.…”

“…In addition to its high efficacy in sheep and cattle against mature and immatureF asciolahepatica, 3' -chloro-4' -(p-chlorophenoxy)-3, 5-diiodosalicylanilide (rafoxanide) (LIX) is active against Hymenolepis nana and H. diminuta in experimentally infected rodents [142].…”

“…As part of a programme aimed towards the development of a fasciolicide suitable for use against both mature and immature liver flukes, more than 200 phenoxysalicylanilides were prepared for screening by workers at the Merck Institute [142,[215][216][217]. To date, structure-activity relationships within the series do not appear to have been published, although the most promising compound 3' -chloro-4' -(p-chlorophenoxy)-3, 5-diiodosalicylanilide (rafoxanide) (LIX) has since been introduced into veterinary medicine [142].…”

N‐(2‐hydroxyaryl)benzamide synthesis from 2‐nitroaryl benzoates via an indium‐mediated reduction‐migration reaction

“…Benzamide derivatives and their analogs are an important class of compound that exhibit various biological effects, such as antihelmintic, antihistaminic, antifungal, and antibacterial activity [1][2][3][4][5][6]. In particular, N-(2-hydroxyphenyl)benzamide derivatives have been synthesized and studied as possible metabolites of antimicrobial benzoxazoles [7][8][9][10][11].…”

Triphenylphosphine catalyzed vinyl amination: A mild, chemospecific and general vinyl amide synthesis

“…1,2 Some derivatives of amides exhibit biological properties such as antihelmintic, antihistamine, antifungal and antibacterial 3-7 . 6-N-(2-Hydroxy-3,5-dichlorophenyl)-2-hydroxy-3,5,6-trichlorobenzamide(oxyclozanide) was discovered in 1969 as an antihelmintic agent effective against Fasciola hepatica for the treatment of liver fluke infection 3 . 3,4-Dihydroxy-6-(N-ethylamino)benzamide is a natural product that has been found in green pepper (Piper nigrum L.) which demonstrated antibacterial activity 5 .…”