title: Chemical modification of nodulisporic acid A: preliminary structure-activity relationships.
abstract: Medicinal chemistry efforts were initiated to identify the key constituents of the nodulisporic acid A (1) pharmacophore that are integral to its potent insecticidal activity. New semisynthetic derivatives delineated 1 into 'permissive' and 'nonpermissive' regions and led to the discovery of new nodulisporamides with significantly improved flea efficacy.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. peter_meinke@merck.com
authors.forename: P T
authors.initials: PT
authors.lastname: Meinke
authors.forename: M B
authors.initials: MB
authors.lastname: Ayer
authors.forename: S L
authors.initials: SL
authors.lastname: Colletti
authors.forename: C
authors.initials: C
authors.lastname: Li
authors.forename: J
authors.initials: J
authors.lastname: Lim
authors.forename: D
authors.initials: D
authors.lastname: Ok
authors.forename: S
authors.initials: S
authors.lastname: Salva
authors.forename: D M
authors.initials: DM
authors.lastname: Schmatz
authors.forename: T L
authors.initials: TL
authors.lastname: Shih
authors.forename: W L
authors.initials: WL
authors.lastname: Shoop
authors.forename: L M
authors.initials: LM
authors.lastname: Warmke
authors.forename: M J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: M
authors.initials: M
authors.lastname: Zakson-Aiken
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
mesh_terms: D000818:Animals; D015195:Drug Design; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D007306:Insecticides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D005423:Siphonaptera; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D007306:Insecticides; C110703:nodulisporic acid A