Anti-parasitic

Alarcon, J.B., Waine, G.W. and McManus, D.P. (1999) DNA vaccines technology and application as anti-parasite and anti-microbial agents. Advances in Parasitology 42, 344-410. 

Pritchard, D.I., Williams, D.J., Behnke, J.M. and Lee, T.D.G. (1983) The role of IgGl hypergammaglobinaemia in immunity to the gastrointestinal nematode Nematospiroides duhius. The immunochemical purification, antigen specificity, in vivo anti-parasite effect of IgGl from immune serum. Immunology 49, 353-365. 

Neurobiology of Nematode Muscle Ligand-gated Ion-channels and Anti-parasitic Drugs... 

Kubicek S, Jenuwein T (2004) A crack in histone lysine methylation. Cell 119 903-906 Kwon HJ, Kim JH, Kim M, Lee JK, Hwang WS, Kim DY (2003) Anti-parasitic activity of depudecin on Neospora caninum via the inhibition of histone deacetylases. Vet Parasitol 112 269-276 Lau OD, Kundu TK, Soccio RE, Ait-Si-Sli S, Khail EM, Vassilev A, Wolffe AP, Nakatani Y, Roeder RG, Cole PA (2000) HATs off Selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell 5 589-595... 

Key words alkaloids, antimicrobial activity, anti-parasitic activity, biology, cytotoxicity, DNA, endogenous security mechanism, estrogenic effect, evolution, genes, haemoglobinization, immune system, inhibitor, locoism, narcotics, regulation, stimulator... 

For a synthesis of the anti-cancer drug taxol TPAP/NMO was used in three steps, two for oxidation of primary alcohols to aldehydes (by TPAP/NMO/PMS/ CHjClj) and one for a secondary alcohol to ketone (by TPAP/NMO/PMS/CHjClj-CHjCN) [66], cf. also [111] and for the SERCA inhibitor thapsigargin (two primary alcohol and one secondary alcohol oxidation steps) [112], This system was also used during synthesis of the cholesterol biosynthesis inhibitor 1233A [52], the antibiotic and anti-parasitic ionophore tetronasin [113, 114] and for the cytotoxic sponge alkaloids motopuramines A and B [115]. 

Several syntheses of natural products and pharmaceuticals involving the conversion of secondary alcohols to ketones using TPAP/NMO/PMS/CH Clj or TPAP/NMO/ PMS/CH3CI3 have been reported. A key early example using TPAP/NMO/PMS/ CH3CI3 for conversion of a secondary alcohol to a ketone intermediate was for the anti-parasitic avermectin-Bla (Fig. 2.6 cf. 1.11) [81,167],... 

Oxamniquine had good anti-parasite activity, especially versus South American strains, and that was relatively free of side effects. 

C. Doerig (2004). Protein kinases as targets for anti-parasitic chemotherapy. Biochim. Biophys. Acta 1697 155-168. 

Nirofuran compounds are also effective anti-parasitic drugs. Nifurtimox, for example, is used to treat Chagas disease (caused by Trypansoma cruzi) but has side effects. In exploring the use of alternatives to nifurtimox, Olea-Azar et al. have examined radical formation from two analogues. Radical anions were observed upon electrolytic reduction of the compounds and a nitroxide, believed to be the glutathionyl radical-adduct, was detected upon electrolysis in the presence of DMPO and GSH. Radical adducts were also detected upon incubation of one of the analogues with microsomes from T. Cruzi.m A novel endo-peroxide reductase has been isolated from T. Cruzi. Whereas the flavoenzyme was found to reduce quinones to their semiquinones, nifurtimox underwent a direct, two-electron reduction, without the formation of radicals.129... 

Excretion from treated animals is yet another source of APIs in the environment. The application of manure as fertilizer is the main source of such veterinary pharmaceuticals into the environment. These APIs can be washed into the surface water by rainfall either after the application of manure or after the direct application of pharmaceuticals on to animals (e.g. anti-parasites). 

Roundworms [ANTI PARASITIC AGENTS - ANTHELMINTICS] (Vol 3) veterinary drugs against [VETERINARY DRUGS] (Vol24)... 

The end of patent cover for most of the modern anthelmintics means that market prices have fallen and therefore funds are lower for investment in research into animal health by pharmaceutical companies. As it is the animal health market that drives any search for anti-parasitic drugs by the pharmaceutical companies, few companies are now looking for modern anti-nematodal drugs and the market size for drugs that kill trematodes and cestodes are such that a search for new drugs cannot be financially justified. Unless a novel anthelmintic that kills nematodes happens to have activity against trematodes or cestodes, it is unlikely that new drugs will become available... 

Both mebendazole and albendazole are used in the long-term treatment of infections and an overall success rate of 97% has been obtained. Albendazole may be the preferred drug as it is cheaper and easier to take than mebendazole (Reuter et al., 2000). Using nitazoxanide with albendazole in a murine model suggests that there may be improved anti-parasitic activity (Stettler et al., 2004). 

Stettler, M., Rossignol, F., Fink, R., Walker, M., Gottstein, B., Merli, M., TheuriMat, R., Thorman, W., Dricot, E., Segers, R. and Hemphill, A. (2004) Secondary and primary murine alveolar echinococcosis combined albendazole/nitazoxanide chemotherapy exhibits profound anti-parasitic activity. International Journal for Parasitology 34, 615-624. 

White, A.C. Jr (2001) Nitazoxanide an important advance in anti-parasitic therapy. American journal of Tropical Medicine and Hygiene 58, 382-383. 

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