Dutton C J, Gibson S P, Goudie A C, Holdom K S, Pacey M S, Ruddock J C, Bu'Lock J D, Richards M K
Central Research Division, Pfizer Ltd., Kent, England.
J Antibiot (Tokyo). 1991 Mar;44(3):357-65. doi: 10.7164/antibiotics.44.357.
Avermectins with a wide range of novel C-25 substituents have been prepared by feeding carboxylic acids or their biosynthetic precursors to a Streptomyces avermitilis mutant strain ATCC 53568. This organism lacks the ability to form isobutyric and S-2-methylbutyric acids from their 2-oxo acid precursors and thus is unable to produce natural avermectins unless supplied with these acids. The novel avermectins produced by mutational biosynthesis possess broad-spectrum antiparasitic activity.
通过向阿维链霉菌突变株ATCC 53568投喂羧酸或其生物合成前体,制备了具有多种新型C-25取代基的阿维菌素。该菌株缺乏从2-氧代酸前体形成异丁酸和S-2-甲基丁酸的能力,因此除非供应这些酸,否则无法产生天然阿维菌素。通过突变生物合成产生的新型阿维菌素具有广谱抗寄生虫活性。