Anthelmintic agent

A phenylacetonitrile derivative, closantel (41), is an anthelmintic agent useful against sheep liver flukes. Its patented synthesis involves a Schotten-Baumann amidation... 

A number of muscle relaxants are useful anthelmintic agents. They cause the parasites to relax their attachment to t he gut wall so that they can be eliminated. One such agent s carbantel 9), Its synthesis follows the classic pattern of r eaction of 4-chlorophenyl isocyanate with ji -amylamidine. ... 

To prepare another such analogue, ]i-methylation of N.,N -dicarbomethoxythiourea gives 10, which itself reacts with complex aniline analogue 21 O ve the veterinary anthelmintic agent felsantel (12). ... 

Reaction of aminothiophenol 97 with reagent 98 obtainable from phenyl urea and thiophosgene leads directly to the anthelmintic agent frentizole (99). In... 

In a somewhat similar vein, alkylation of the urea derivative 109 with methyl iodide affords the S-methyl ether 110. Condensation of that with taurine (111), leads to the guanidine 112, again by an addition elimination process. The product is the anthelmintic agent netobimin (112) [271. 

Nucleophilic aromatic substitution of the anion from ary lace ton itrile 113 on the dichloroni-trobenzene 114 results in replacement of the para halogen and formation of 115. Reduction of the nitro group gives the corresponding aniline (116). Acylation of the amine with 3,5-diiodoacetylsa-licylic acid 117 by means of the mixed anhydride formed by use of ethyl chloroformate, gives, after alkaline hydroly.sis, the anthelmintic agent closantel (118) [28]. 

An analogous sequence leads to the anthelmintic agent, etibendazole (50). Reaction of the benzophenone 47, which can be obtained by acylation of o-nitroaniline with g-fluorobenzoyl chloride, with ethylene glycol leads to acetal 48. Sequential reduction of the nitro group and cyclization of the resulting diamine (49) with N,N-dicarbomethoxy-S-methylthiourea gives the benzimidazole etibendazole (50) fl6]. 

One of the more interesting syntheses for the anthelmintic agent praziquantel (123)... 

Anthelmintic agents have been utilized to treat a multimde of nematode infections. These include roundworms, tapeworms, and lungworms in cattle and swine. Two classes of compounds included as anthelmintic agents will be discussed here, lev-amisole and thiabendazoles (thiabendazoles can also act as pesticides). Thiabendazoles can cause nephrotoxicity, teratogenesis, and immunosuppression and can disrupt endocrine balance. Because of these toxicides, residues of these compounds in food animals are of food safety concern. 

The quaternary ammonium salt 73, thenium closylate, is an anthelmintic agent. Many substances of this general type are effective by interfering with nervous conduction, and thereby muscle tone, of intestinal worms. This allows their expulsion, not... 

Burg, R.W., Miller, B.M., Baker, E.E. et al. (1979) Avermectins, new family of potent anthelmintic agents producing organism and fermentation. Antimicrobial Agents and Chemotherapy, 15, 361-367. 

A review discussing anthelmintic activity, pharmacokinetics, toxicity, side effects, and clinical use of niclosamide and other anthelmintic agents is reported [95],... 

Compound 331 was prepared using the free amino acid derived by coupling the product between proline and a substituted tryptophan. It was employed for studies on the biosynthesis of the anthelmintic agent paraherquamide <2001T5303>. Compound 332 was obtained by TFA-mediated reaction from the corresponding NH-/-Bu dipeptide... 

Dibenzothiophene, its sulfoxide, and its sulfone are inactive as anthelmintic agents against Syphacia obvelata and Aspiculuvis... 

This dual activity against both nematode and arthropod parasites of animals was an unexpected bonus from a screen for anthelmintic agents. The reason for this broad activity lies in their mode of action. They act by interfering with y-aminobutyric acid (GABA) mediated neurotransmission. When treated with avermectin, the nematode Ascaris suum becomes paralyzed although it retains normal muscle tone (17). Picrotoxin, an antagonist of GABA, can reverse the effect of avermectin on neurotransmission vitro. 

Anthelmintic agents, 68-69 Antibacterial feed additives, synthetic and antibiotic, 3t Antibacterial therapy, objective, 12 Antibiotic combinations, advantages and disadvantages, 21... 

The anthelmintic agent levamisole increases delayed hypersensitivity and T-cell mediated immunity. It has been used as adjuvant therapy for colorectal cancer. A recent Cochrane review concluded that... 

Mechanism of Action An anthelmintic agent that inhibits helminth-specific mitochondrial fumarate reductase. Therapeutic Effect Suppresses parasite production. Pharmacokinetics Rapidly and well absorbed from the gastrointestinal (Gl) tract. Rapidly metabolized in liver. Primarily excreted in urine partially eliminated in feces. Half4ife 1 2 hr... 

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