![]() Further studies are required to elucidate the role of this enzyme in the mode of action of mefloquine. Affinity chromatography employing epoxy-sepharose-bound mefloquin and extracts of HFF resulted in the pull-down of nicotinamide phosphoribosyltransferase (accession no NP_005737) as a mefloquine-binding protein (authors, unpublished data). Therefore, a target in human cells should exist. gondii tachyzoites cultured in human foreskin fibroblasts, however, the therapeutic window is very small ( Müller and Hemphill, 2011a). Mefloquine inhibits the proliferation of N. Mefloquine and other quinolines inhibit various protein kinases but at relatively high concentrations ( Wang et al., 1994). Thus, for mefloquine, there must be other targets besides heme degradation. but also against Schistosoma mansoni adult worms, where it inhibits the formation of hemozoin, a heme detoxification aggregate ( Oliveira et al., 2004), and against juvenile stages ( Keiser et al., 2009). Mefloquine is effective not only against Plasmodium sp. Their mode of action is reported to rely on the interference with hemoglobin digestion by the parasite ( Foley and Tilley, 1998). The quinolines mefloquine, chloroquine and related compounds are well-established antimalarials ( Brocks and Mehvar, 2003 Milner et al., 2010). Joachim Müller, Andrew Hemphill, in International Review of Cell and Molecular Biology, 2013 4.2 Mefloquine, Another Compound with Different Targets Of these, decoquinate is a highly effective and well tolerated drug that can be used to prevent coccidiosis ( Eimeria spp.) in chickens at a dose of 30 mg/kg. ![]() Two other hydroxyquinoline drugs that need to be mentioned here are decoquinate ( 81) and buquinolate ( 82), which find use in the treatment of coccidiosis in poultry. ![]() emerging clamoxyquin ( 80) as a powerful drug for treating various forms of amoebisis in animals and man. Consequently a wide range of Mannich bases derived from 8-hydroxyquinolines were synthesized by Helin and Vander Werf and Burckhalter et al. ĭemonstration of high amoebicidal activity associated with 79 established the fact that introduction of an aminomethyl chain at 7-position of 8-hydroxyquinolines provides compounds with potent activity against E. The most effective compound was found to be 7-(N,N-diethylaminomethyl)-5-chloro-8-hydroxyquinoline ( 79), which exhibited activity against intestinal amoebiasis in man. Ī Mannich reaction with 5-halo-8-hydroxyquinolines has led to a series of 7-aminomethyl-5-halo-8-hydroxyquinolines with potent in vitro and in vivo activity against E. However, the three iodinated 8-hydroxyquinolines namely chiniofon ( 74), vioform ( 75) and embequin ( 76) have been extensively used to treat intestinal amoebiasis in human. The 2-methyl derivative of 75 called chloroquinaldol ( 78) has also been found to be effective against intestinal amoebiasis in human. Later, these halogenated 8-hydroxyquinolines were found to possess strong amoebicidal properties. Substitution of the sulphonate moiety in chiniofon ( 74) by halogens resulted in the synthesis of 5-chloro-7-iodo-8-hydroxyquinoline ( 75, clioquinol,vioform), 5,7-diiodo-8-hydroxyquinoline ( 76, embequine, diiodohydroxyquinoline), and broxyquinoline ( 77). In fact, a random screening programme of halogenated quinolin-8-ols for search of antiseptic agents led to the discovery of sodium 7-iodo-8-quinolinol-5-sulphonate ( 74, chiniofon). However, their value as antiseptic agents was established long before their amoebicidal properties were discovered. ![]() Quinoline derivatives are amongst the earliest drugs used to treat amoebiasis. Satyavan Sharma, Nitya Anand, in Pharmacochemistry Library, 1997 6 HYDROXYQUINOLINES ![]()
0 Comments
Leave a Reply. |
AuthorWrite something about yourself. No need to be fancy, just an overview. ArchivesCategories |