Parasiticidal compounds

5-Amino-3-cyano-l-(2,6-dichloro-4-trifluoromethylphenyl)pyrazole (5.0 g) was dissolved in 60ml acetonitrile at ambient temperature and N-iodosuccinimide (3.52 g) added portion wise over 5 minutes. The mixture was stirred 1 hour, concentrated, and this crude 

5-Amino-3-cyano-l-(2,6-dichloro-4-trifluoromethylphenyl)-4-trimethylsilyl-ethynlpyrazole 

To the crude product from Step 1 (6.96 g) dissolved in 30 ml triethylamine and 6 ml dimethylformamide at ambient temperature was added 3 ml trimethylsilylacetylene, Cul (150 mg) and bis(triphenyl-phosphine)palladium(II)chloride (300 mg). The mixture was heated 1 hour to 50-60°C, an additional 0.3 ml trimethylsilylacetylene added, and heating continued 30 minutes. The cooled mixture was diluted with 250 ml water, extracted with 250 ml diethyl ether, separated, dried, and concentrated. The material was purified by chromatography on silica gel using CH2Cl2/hexane, 1 1, re-crystallized from diethyl ether/hexane, and the product isolated, mp = 181-182°C. H-NMR, MS, and elemental analysis data supplied. 

The preparation of the Step 1 reagent is described by the author and elsewhere (1). 

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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). 

Thiirane is more bactericidal than oxirane, and derivatives of 2-mei captomethylthiirane inhibit tuberculosis. The following pharmacological uses have been reported for compounds derived from thiirane derivatives gold complexes of the adducts of diethylphosphine and thiirane (antiarthritic), adducts of thiiranes and malononitrile (antibacterial, blood vessel dilators, muscle relaxants, sedatives), thermolysis products of thiirane 1-oxides and adducts of thiirane 1-oxides with sulfenyl chlorides (antibacterial), adducts of 2,3-diarylthiirene 1,1-dioxides with ynamines (antibacterial, parasiticidal), adducts of 2,3-diarylthiirene 1,1-dioxides with enamines (antifertility), adducts of p-aminophenylacetic esters with thiirane (immunosuppressants), adducts of amines and thiiranes (radioprotective drugs). 

The term pharmaceutical includes more than 4,000 chemicals used to control and treat different kinds of diseases in humans and animals. Pharmaceuticals include analgesics, anti-inflammatories, anti-epileptics, (l-blockers, compounds used to prevent and treat parasites and microbial infections (parasiticides and antibiotics) and those for combating cancer. Hormones are also a class of pharmaceuticals but due to their particular involvement in endocrine disruption, they have been discussed in a separate section (see above). 

As the causative parasites for these diseases are closely related, and the genome of each has been sequenced, it is not surprising that a number of common biochemical pathways have been targeted by drug discovery efforts [6]. In addition, screening for parasiticidal activity of compounds has frequently been performed simultaneously against representative strains of the three major parasites, hence many of the chemotypes described in this chapter exhibit activity against all three. 

Thus, in the year 1950, an inventor named Tolkmith (IS) presented a patent application claiming a certain methane phosphonic chloride. The only utility stated for the compound was that it was of value as an intermediate for the preparation of more complex phosphorus derivatives and as a constituent of a parasiticide. The Patent Office Board of Appeals in its decision, held that the applicant s showing of utility did not comply with Section 112 of the patent statutes requiring that the manner and process of making and using the invention be described in such exact terms as to enable one skilled in the art to make and use the same. The board went on to say ... 

Thus, an array of bioactive compounds, often derived directly from the pharmaceutical and crop protection industries, are used antibacterials, anticoccidials, miticides, nematicides, parasiticides (for control of both internal and external parasites), and insecticides. In addition, other specialty chemicals, such as growth-regulating, estrous-synchronizing, and nutrient-repartitioning agents, are in use and are being considered for use in animal production. 

THERAP CAT (VET) As a component of Compound Benzoin Tincture. Has been used as a parasiticide. 

The CM compounds arc esters of carbamie acid. Unlike OPs, CM compounds are not structurally complex. CMs are used as pesticides in agricultural crops and gardens, as therapeutic drugs in human medicine (Alzheimer s disease, myasthenia gravis, glaucoma, and in prophylaxis of OP nerve gas poisoning), and in veterinary medicine (as parasiticides). 

The same scheme has been adopted for the determination of several antibacterials (quinolones and erythromycin A), fungicides, and parasiticides in salmon tissue. In this case, samples were extracted with acidic ACN, and then dSPE was carried out with a Bondesil NH2 sorbent, followed by LC-TOE-MS determination. Excellent recoveries were obtained with the exception of enrofloxacin (40%), although matrix suppression effects were observed for most of target compounds. ... 

Arsenic is traditionally, closely linked to homicides and suicides. Its toxicity has to do with the chemical form of this element. Hence, inorganic compounds of arsenic are more toxic, followed by organic compounds and finally arsenic in gas form. " During the past, products based on arsenic such as parasiticides, insecticides, fungicides, wood preservatives, and other similar products were widely used. Nowadays, all the above are forbidden in many countries due to the proved toxicity of arsenic. 

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