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

作者：Mack Daniel J; Isoe Jun; Miesfeld Roger L^*; Njardarson Jon T

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(16): 5177-5181.

DOI：10.1016/j.bmcl.2012.06.076

• Golgicide A
• Malaria
• Mosquito
• COPI
• GBF1

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.

• 出版日期2012-8-15