CAS: 18174-72-6; Muscimol Hbr

📜3-(Phenylmethoxy)-5-Isoxazolemethanamine置于氢溴酸体系中,用 溶剂黄146 用作溶剂,化学反应 24.0H,以179 Mg的收率获得蝇蕈醇溴酸盐
参考文献:4,5-Substituted 3-Isoxazolols With Insecticidal Activity Act As Competitive Antagonists Of Housefly Gaba Receptors
标题:4,5-Substituted 3-Isoxazolols With Insecticidal Activity Act As Competitive Antagonists Of Housefly Gaba Receptors
摘要:The Insect Gaba Receptor (Gabar),Which-Is Composed Of Five Rdl Subunits,Represents An Important Target For Insecticides. A Series Of 4,5-Disubstituted 3-Isoxazolols,Including Muscimol,Analogues; Were Synthesized And Examined For Their Activities Against Four Splice Variants (Ac,Ad,Bc,And Bd) Of Housefly Gabars Expressed In Xenopus Oocytes. Muscimol Was A More Potent Agonist Than Gaba In All Four Splice Variants,Whereas Synthesized Analogues Did,Not Exhibit Agonism But Rather Antagonism In Housefly Gabars. The Introduction Of Bicyclic Aromatic Groups At The 4-Position Of Muscimol And The Simultaneous Replacement Of The Aminomethyl Group With A Carbamoyl Group At The 5-Position To Afford Six 4-Aryl-5-Carbamoyl-3-Isoxazolols Resulted In Compounds That Exhibited Significantly Enhanced Antagonism With Ic50 Value In The Low Micromolar Range In The Ac Variant. The Inhibition Of Gaba-Induced Currents By 100 Mu M Analogues Was Approximately 1.5-4-Fold Greater In The Ac And Bc Variants Than In The Ad And Bd Variants. 4-(3-Biphenylyl)-5-Carbamoyl-3-Isoxazolol Displayed Competitive Antagonism,With Ic50 Values Of 30,34,1:07,And 96 Mu M In The Ac,Bc,Ad,And Bd Variants,Respectively,And Exhibited Moderate Insecticidal Activity Against Houseflies,With An Ld50,Value Of 5.6 Nmol/fly. These Findings Suggest That These 3-Isoxazolol Analogues Are Novel Lead Compounds For The Design And Development Of Insecticides That Target The Orthosteric Site Of Housefly Gabars.
Doi:10.1021/acs.Jafc.5B01843