Bihani_2015_Bioorg.Med.Chem.Lett_25_5732

Reference

Title : PPL catalyzed four-component PASE synthesis of 5-monosubstituted barbiturates: Structure and pharmacological properties - Bihani_2015_Bioorg.Med.Chem.Lett_25_5732
Author(s) : Bihani M , Bora PP , Verma AK , Baruah R , Boruah HP , Bez G
Ref : Bioorganic & Medicinal Chemistry Lett , 25 :5732 , 2015
Abstract : Enzymatic four-component reactions are very rare although three-component enzymatic promiscuous reactions are widely reported. Herein, we report an efficient PASE protocol for the synthesis of potentially lipophilic zwitterionic 5-monosubstituted barbiturates by four component reaction of mixture of ethyl acetoacetate, hydrazine hydrate, aldehyde and barbituric acid in ethanol at room temperature. Seven different lipases were screened for their promiscuous activity towards the synthesis of 5-monosubstituted barbiturates and the lipase from porcine pancreas (PPL) found to give optimum efficiency. The zwitterionic 5-monosubstituted barbiturates with pyrazolyl ring showed promising pharmacological activity upon screening for antibacterial and apoptotic properties.
ESTHER : Bihani_2015_Bioorg.Med.Chem.Lett_25_5732
PubMedSearch : Bihani_2015_Bioorg.Med.Chem.Lett_25_5732
PubMedID: 26546212

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Citations formats

Bihani M, Bora PP, Verma AK, Baruah R, Boruah HP, Bez G (2015)
PPL catalyzed four-component PASE synthesis of 5-monosubstituted barbiturates: Structure and pharmacological properties
Bioorganic & Medicinal Chemistry Lett 25 :5732

Bihani M, Bora PP, Verma AK, Baruah R, Boruah HP, Bez G (2015)
Bioorganic & Medicinal Chemistry Lett 25 :5732