title: Synthesis and biological activity of 13-epi-avermectins: potent anthelmintic agents with an increased margin of safety.
abstract: Chemical conversion of the potent anthelmintic natural products avermectin B1 (1) and avermectin B2 (3) to the corresponding 13-epi analogs (15 and 9) is described. The novel analogs retain the full potency of the natural products but are substantially safer.
authors.affiliation: Merck Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.
authors.forename: T A
authors.initials: TA
authors.lastname: Blizzard
authors.forename: G M
authors.initials: GM
authors.lastname: Margiatto
authors.forename: H
authors.initials: H
authors.lastname: Mrozik
authors.forename: W L
authors.initials: WL
authors.lastname: Shoop
authors.forename: R A
authors.initials: RA
authors.lastname: Frankshun
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001156:Artemia; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D012756:Sheep; D013329:Structure-Activity Relationship
chemical_list: D000871:Anthelmintics; D007559:Ivermectin; C019264:avermectin