Antiparasitic compounds

Diethylcarbamazine is an anthelmintic drug that does not resemble other antiparasitic compounds although it has some relationship with piperazine derivatives and it has been useful in the management of filariasis due to Wuchereria bancrofti or Brugia malayi and Loa loa and of tropical eosinophilia. It is a lipoxygenase inhibitor and alters the surface structure of the parasite making it more susceptible to destruction by the host. It is well absorbed and widely distributed. It is eliminated with an half-life of 5-13 hours both by metabolism and excretion unchanged in the urine. 

In the syntheses of fragments of the antiparasitic compounds avermectins or milbemycins selenocycloetherification was used for the construction of a highly substituted hexahydroben-zofuran derivative (Table 8, entry 8)29. The intramolecular cyclization of a cyclohexadienyl hydroxymethyl ketone with phenylselenenyl chloride proceeded stereoselectively in a 1,4-fash-ion resulting in an anti orientation of oxygen and selenium. This was followed by oxidation and rearrangement. 

Perez-Montoto, L.G., Santana, L., Gonzalez-Diaz, H. Scoring function for DNA-drug docking of anticancer and antiparasitic compounds based on spectral moments of 2d lattice graphs for molecular dynamics trajectories. Eur. J. Med. Chem. 2009, 44(11), 4461. 

The avermectins are a family of broad-spectrum antiparasitic compounds with avermectin A (Figure 8.10) being an example. These compounds were originally sold by Merck (with a slight chemical modification) as veterinary agents... 

Treatment of (171) with aqueous alkali and dimethyl sulfate gave the trimethyl derivative (172). The structures of (171) and (172) were proved by x-ray analysis <85JCS(P2)1913> see also <87JOM(325)l53, 90IJC(B)711>. These products and others prepared from substituted anthranilamides were synthesized with a view to the development of antiparasitic compounds <82MI 625-01 >. 

Selectivity of an antiparasitic compound must depend upon its mode of specific inhibition of parasite replication leaving host processes unaffected. In principle, these ents are expected to exert their selective actions against growth of the invadii organisms by having one or both of the following properties ... 

In a subsequent paper, Jacobsen and co-workers utilized hydroxylactams as precursors to a reactive A-acyhminium ion intermediate. Again, a wide variety of substrates were demonstrated using this methodology including the synthesis of (-i-)-harmicine 116 [36], an antiparasitic compound derived from the Malaysian plant Kopsia griffithii (Scheme 1.28) [38]. 

Ziegler HL, Hansen HS, Staerk D, Christensen SB, Hageratrand H (2004) The antiparasitic compound licochalcone a is a potent echinocytogenic agent that modifies the erythrocyte... 

Graziose, R, Rojas-Silva, P, Rathinasabapathy, T, Dekock, C, Grace, MH, Poulev, A., Lila, MA, Smith, P, Raskin, 1. Antiparasitic compounds from Comus florida L. with activies against Plasmodium falciparum and Leishmania tarentalae. J. Ethnopharmacol, 2012, 142, 456-461... 

Wilson WD, Tanious FA, Mathis A, et al. Antiparasitic compounds that target DNA. BiocHmie. 2008 90 999-1014. 

This section includes veterinary applications. The antiviral, bactericidal, and antimicrobial applications of 2-aminothiazoles and 2-imino-4-thiazolines are summarized in Table VI-7. They show a marked anti-trichonomicidal activity, which has even been quantitatively measured by the Hansch approach (797). The antiparasitic action of these compounds has been investigated for some compounds and is summarized in Table VI-8 interesting results were obtained with aminotrozal (1348). 

ANTIPARASITIC AGENTS - ANTIPROTOZOALS] (Vol 3) -inclusion compounds [INCLUSION COMPOUNDS] (Vol 14)... 

In 1912, however, (201) it was discovered that espundia (American mucocutaneous leishmaniasis) can be cured by tartar emetic. It was soon learned that kala-a2ar (visceral leishmaniasis) and oriental sore (a cutaneous form of the disease occurring in the Middle East) also respond to antimonial therapy, especially when compounds of pentavalent antimony are employed. Treatment of leishmaniasis with the latter type of antimonials is safe and effective in over 90% of the cases (202). In 1918, it was demonstrated that tartar emetic is of value in the treatment of schistosomiasis (203). Pentavalent antimonials proved to be less effective. The introduction of antimony compounds for the treatment of parasitic diseases is undoubtedly one of the important milestones in the history of therapeutics (see Antiparasitic agents). 

Because of the outbreak of antimony-resistant leishmania sis and the need to develop an oraky-adrninistered therapy, the use of many other compounds has been considered. Those that appear to have clinical utility ate aHoputinol (62), ketoconazole (63), and both systemicaHy and topically applied paromomycin (8) (see Antiparasitic agents, antimycotics). 

Droncit), C H24N202, for use as a parasiticide. Ivermectic [70288-86-7] and an experimental, pyrethmm-based compound (Py-Sal 25) are both involved ia clinical trials ia Europe to determine if they can control sea Hce on salmon (see Antiparasitic AGENTS, AVERMECTINS). 

Antiparasitic. A general term for compounds that kill protozoan or metazoan infective organisms. 

The antiparasitic drug clorsulon (206), contains a rather unusual trichloroethylene group. This function is established early in the syntliesis by treatment of the perhalogenated compound 203 obtained from reduction of 202 with iron powder. Chlorosulfonation of 204 by means of chloro-sulfonic acid, followed by conver.sion of. sulfonyl chloride 205 to the amide, gives clorsulon (206) 153],... 

There remains an urgent need for new effective antiparasitic agents, an area of drug development that has languished because of poor economic return. The spread of resistance to chloroquine (an antimalaria treatment) is one reason for attention to be paid to this area, as well as the sheer numbers of people affected. Antimony compounds (43) and (44) (Figure 20) are used to treat... 

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