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Chapter: Medicinal Chemistry : Anthelmintics

Natural products : Avermectins (Mectizan) - Synthesis and Drug Profile

Anthelmintics - Synthesis and Drug Profile

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Avermectins (Mectizan)

Mode of action: Avermectins specifically open the chloride channels in the invertebrate system distinct from the GABA-gated and glutamate-gated chloride channels.

Metabolism: It is metabolized and it gives 3-O-demethyl-22,23-dihydroavermectin B1α monosaccharide.

Properties and uses: Avermectins are macrocyclic lactones with broad antinematocidal activity. This class of compound was isolated from a fermentation broth of a soil actinomycetics (Streptomycin avermitils). The drug avermectin is now effectively being used to treat and control onchocera volvulus, the filarial infection responsible for liver blindness. Ivermectin is a mixture of B1a and B1b (80:20) and is prepared by catalytic reduction of ivermectin B1 (Abamectin)

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