Publication | Closed Access
Silver(I)‐Catalyzed Route to Pyrroles: Synthesis of Halogenated Pseudilins as Allosteric Inhibitors for Myosin ATPase and X‐ray Crystal Structures of the Protein–Inhibitor Complexes
21
Citations
45
References
2014
Year
Molecular PharmacologyBiochemistryNatural SciencesMedicineEnzyme CatalysisHalogenated PseudilinsMolecular BiologyAllosteric InhibitorsMyosin Atpase ActivityStructure-function Enzyme KineticsAlkaloids PentabromopseudilinChemical BiologyPharmacologyPharmaceutical ChemistryMyosin AtpaseDrug DiscoveryNatural Product Synthesis
Abstract The pentahalogenated 2‐arylpyrrole‐type alkaloids pentabromopseudilin and pentachloropseudilin represent a new class of isoform‐specific allosteric inhibitors of myosin ATPase. Herein, we describe an application of the silver(I)‐catalyzed cycloisomerization of N ‐(homopropargyl)toluenesulfonamides to the total syntheses of these natural products and several non‐natural analogues. Moreover, we examine the inhibitiory effect of pentahalogenated pseudilins on myosin ATPase activity.
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