Binding of 3‐Alkyl‐1,4‐benzodiazepin‐2‐one Stereoisomers to Human Serum Albumin

Ilona Fitos, Miklós Simonyi, Zsuzsanna Tegyey, Márton Kajtár, László Ötvös

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

The binding of both enantiomers of 3‐alkyl‐1,4‐benzodiazepin‐2‐ones to human serum albumin (HSA) strengthens with increasing size of the 3‐alkyl substituent. 3,3‐Dimethylderivatives show diminished binding affinities although they bind in the favourable conformation assumed by the (S)‐enantiomers. N(1)‐Methyl substitution increases the enantioselectivity of binding by selectively enhancing the binding strength of (S)‐antipodes.

Original languageEnglish
Pages (from-to)744-749
Number of pages6
JournalArchiv der Pharmazie
Volume319
Issue number8
DOIs
Publication statusPublished - 1986

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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