α-Substitution effects on the ease of S → N-Acyl transfer in aminothioesters

Bahaa El Dien M. El-Gendy, Ebrahim H. Ghazvini Zadeh, Ania C. Sotuyo, Girinath G. Pillai, Alan R. Katritzky

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

In S-acylcysteines and homocysteines, the efficacy and rate of S → N-acyl transfer (5 and 6 cyclic TSs) vary with the size of S-acyl group. Conformational and quantum chemical calculations indicate that the spatial distance, b(N-C), between the terminal amine and the thioester carbon is shortened by α-C(O)X (X=OH, OMe, NH2) substituents. Spatial distance, b(N-C), between the terminal amine and the thioester carbon is shortened by α-C(O)X (X=OH, OMe, NH2) substituents.

Original languageEnglish
Pages (from-to)577-582
Number of pages6
JournalChemical Biology and Drug Design
Volume81
Issue number5
DOIs
StatePublished - May 2013

Keywords

  • Aminothioesters
  • Conformational analysis
  • S→N-acyl transfer

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