Distinct biological effects of golgicide a derivatives on larval and adult mosquitoes

Daniel J. MacK, Jun Isoe, Roger L. Miesfeld, Jon T. Njardarson

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

A collection of Golgicide A (GCA) analogs has been synthesized and evaluated in larval and adult mosquito assays. Commercially available GCA is a mixture of four compounds. One enantiomer (GCA-2) of the major diastereomer in this mixture was shown to be responsible for the unique activity of GCA. Structure-activity studies (SAR) of the GCA architecture suggested that the pyridine ring was most easily manipulated without loss or gain in new activity. Eighteen GCA analogs were synthesized of which five displayed distinct behavior between larval and adult mosquitos, resulting in complete mortality of both Aedes aegypti and Anopheles stephensi larvae. Two analogs from the collection were shown to be distinct from the rest in displaying high selectivity and efficiency in killing An. stephensi larvae.

Original languageEnglish (US)
Pages (from-to)5177-5181
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number16
DOIs
StatePublished - Aug 15 2012

Keywords

  • COPI
  • GBF1
  • Golgicide A
  • Malaria
  • Mosquito

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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