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

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.