Anthelmintic activities

Able to form Ag salt of lower solubility than AgQ in H2O. Therefore applications in photographic processes Inhibition of histidine decarboxylase activity Antifoggant for color films Anthelmintic activity Quenching for oil composition caialj si for the industrial isomerization of cis a, (3 unsaturaied carboxylic acids rubber vul-cankzate improver... 

Phiorog1iicino1-3,5-dimethyl-1-(2-amino-3-hydroxyhutyryl)ether is characterized by antiarrhythmic activity (176). 2,4-Diacylphloroglucinols were patented as compounds with pronounced anthelmintic activity (177). Phloroglucinol mono- and di-(2-chloroethyl) ethers have antispasmodic or tranquilizing activities (178). 2-(3,5-DiaLkoxyphenoxy)ethylamines have antispasmodic, choloretic, sedative, and vasodilating effects (179). 

Derivatives Containing a 5-Monosubstituted-2-deoxystreptamine Moiety. Few derivatives of this type are known. One is hygromycin B (15) isolated from Streptomjces hjgroscopicus and Streptomjces eurocidicus (131—133). The antibacterial activity is poor, but hygromycin B is reported to have anthelmintic activity (see AnTIPARASITIC AGENTS, ANTHELMINTICS). 

Levamisole. The racemic mixture of the d and / isomers of tetramisole [6649-23-6] was first described in 1966. It is used as an anthelmintic against a wide variety of nematodes, including lungworms, of mminants, swine, horses, dogs, and poultry. Anthelmintic activity resides in the /-isomer, levamisole [14769-73-4], the form used. 

Piperazine Salts. Pipera2ine citrate is highly effective against bothM. lumbricoides (large roundworm) and E. vermicularis (pinworm). A large number of substituted pipera2ine derivatives exhibit anthelmintic activity however, only diethylcarbama2ine (9) is used clinically (26). 

Triazole-4-carboxylic acid, 5-anilino-anthelmintic activity, 5, 732... 

Several isothiazolyl derivatives (38) are included in a series of benzimidazoles claimed to have anthelmintic activity. ... 

A number of amidines have anthelmintic activity. Bunamidine (25), indicated for treatment of human pinworm infestations, is prepared from a-naphthylhexyl-ether (23) by Friedel-Crafts type reaction with cyanogen bromide and aluminum chloride to give nitrile (24). This, then, is reacted with the magnesium bromide salt of di-n-propylamine leading to the naph-thamidine structure (25). -... 

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

Akhtar, M. S., Iqbal, Z., Khan, M. N. and Lateef, M. (2000). Anthelmintic activity of medicinal plants with particular reference to their use in animals in the Indo-Pakistan subcontinent . Small Ruminant Research, 38, 99-107. 

Githiori, J. B., Hoglund, J. Waller P. J. and Baker, R. L. (2002). Anthelmintic activity of preparations derived from Myrsine africana and Rapanea melanophloeos against the nematode parasite , Haemonchus contortus, of sheep. Journal of Ethnopharmacology, 80(2-3), 187-191. 

Pessoa, L. M., Morais, S. M., Bevilaqua, C. M. L. and Luciano, J. H. S. (2002). Anthelmintic activity of essential oil of Ocimum gratissimum Linn, and eugenol against Haemonchus contortus. Veterinary Parasitology, 109, 59-63. 

Several reports are available on the biological activities of thioamide derivatives. The thioamide derivatives have shown significant activities, such as antituberculosis drug, anti-influenza virus activity, antitumor activity, anthelmintic activity, opioid receptor binding property, etc.94 101... 

C02H >j C02H Red algae -D/genea simplex a-Kainic acid - nonprotein amino acid with anthelmintic activity 230, 255... 

A number of other fermentation products have been reported to have anthelmintic activity. Among these are the aminoglycoside, G-418, the destomycins, paromomycin, anthelvencin, aspiculamycin, anthelmycin, and the axenomycins. However, none of these has seen commercial use. 

Further experience has demonstrated that it was not solely the choice of assay but the great good fortune to have received a group of cultures from the Kitasato Institute and to have made the decision to screen these cultures in the dubius assay. One of these cultures, OS-3153, was active. The screening of several tens of thousands of soil isolates in this assay has failed to detect any remotely similar anthelmintic activity. Of the fermentation products discussed, this is the only one where the activity for which the product was eventually marketed was found by direct screening. (Zeranol might be considered to be another example, but it was not discovered by screening.)... 

The microorganism was classified as a new species of actinomycete. Streptomyces avermitilis. Its anthelmintic activity was shown to reside in 8 closely related macrocyclic lactones, named avermectins, which were also found to possess activity against free-living and parasitic arthropods. One of the natural components, avermectin is now being evaluated as a pesticide for the control of mites of citrus and cotton crops and control of the Red Imported Fire Ant. A chemical derivative, 22,23-dihydroavermectin or ivermectin, has been developed as an antiparasitic agent. It is being marketed for use in cattle, horses and sheep and is expected to become available for swine and dogs. 

Several vitro assays for detecting fermentation products with anthelmintic activity had been run without success, primarily because of the large number of toxic compounds which had to be eliminated. Finally, the decision was made to use an vivo assay in mice with the hope that the mice would screen out the non-specific toxic compounds. 

In the third test, the activity was titrated using serial 2-fold dilutions. All four levels were fully active, and this time there was little sign of toxicity. A few cultures had been confirmed active previously, but none had exhibited a separation of toxicity from activity, let alone activity over at least an 8-fold range. After an Inauspicious start, the activity of culture OS-3153 had been firmly established. Success had been achieved in the quest for a fermentation product with anthelmintic activity. In fact, as events would soon prove, the newly found product had an even broader activity than had been anticipated. 

Based on a correlation of anthelmintic activity and HPLC analysis of the total avermectin complex, it was estimated that the third fermentation contained a minimum of 9 pg/ml. Improvement of the medium increased the yield by the original culture (MA-4680) to 120 yg/ml. A high-producing isolate (MA-4848) obtained from this culture produced nearly 500 pg/ml of total avermectins. Thus, this culture yielded readily to medium improvement and isolate selection to produce relatively large amounts of the avermectins. Accounts of the early fermentation studies and taxonomy have been published (1-2). 

PHARMACOLOGICAL ACTIVITIES AND CLINICAL TRIALS Alkaline phosphatase stimulation. Extract of the leaf, administered orally to adults, was active. Patients with subacute hepatic necrosis had negative workup, except for consumption of 15 tablets of the herbal extract per day for 4 months L Anthelmintic activity. Water and petroleum ether extracts of the dried oleoresin were active on Eimeria tenella in chicken - . Anti-amoebic activity. The resin of Larrea produced inhibitory activity at a concentration of 1 ppm on Entamoeba invadens PZ axenic cultures. The nordihydroguaiaretic acid activity was observed at 10" to 10" concentrations - . 

Anthelmintic activity. Saline extract of the dried rhizome, at a concentration of 2.5%, was 100% effective on Anisakis species larvae " . 

Through the reaction of 2-bromoquinolizinium ion or its 1-acetoxy analog with suitable amines, Alaimo and coworkers have produced a large number of 2-aminoquinolizinium salts having useful medicinal activity. Most, but by no means all, of these active compounds are 2-arylaminoquinolizinium salts (219 and 220). Best anthelmintic activity was found in (219) when R2 was alkoxy (< Bu) or dialkylamino (NMe2 or NEt2) and R3 = H (70JMC554). 

It is a synthetic benzimidazole having a wide spectrum of anthelmintic activity. After administration it is poorly absorbed and approximately 90 percent of the drug is passed in faeces. Complete clearance of the parasites from the GIT may take up to three days. 

Compound 56 [39] was heated under refluxing in xylene to give rearranged product 63 in good yield. Compound 63 was subjected to conditions described by Williams [46] to provide 65 in low yield. Compound 65 did not show ant anthelmintic activity. ... 

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