Process for production of avermectins and cultures therefor

C - Chemistry – Metallurgy – 12 – P

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C12P 19/62 (2006.01) A01N 43/90 (2006.01) C07H 19/01 (2006.01) C12N 1/20 (2006.01)

Patent

CA 1338141

Novel mutant strains of Streptomyces avermitilis are produced by mutation of avermectin-producing S. avermitilis strains. The novel strains lack branched-chain amino acid transaminase activity and/or branched-chain 2-oxo acid dehydrogenase activity or they lack branched-chain 2-oxo acid dehydrogenase activity and avermectin B O-methyltransferase activity. These novel strains are useful for the production of both natural and non-natural avermectins which can be used as parasiticides. The avermectins have the formula: (I) Image (wherein the broken line at the 22-23 position represents an optional double bond; R1 is H or OH when the double bond is absent, or is H when the double bond is present. R is isopropyl or (S)-sec-butyl when the avermectins are natural and is other than isopropyl or (S)-sec-butyl when the avermectins are non-natural, such as alkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl or heterocyclic ring R2 is a disaccharide moiety of the formula: Image [wherein each of R4 and R5 is hydrogen or methyl]; and R3 is hydrogen or methyl).

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