GENERAL-APPROACH TO CHIROPTICAL CHARACTERIZATION OF BINDING OF PROCHIRAL AND CHIRAL 1,4-BENZODIAZEPIN-2-ONES TO HUMAN-SERUM ALBUMIN

General interpretation of chiroptical characteristics of binding process of prochiral (Z) and chiral (Z*) 1,4-benzodiazepin-2-ones to human serum albumin (HSA) is presented. Interpretation of binding of Z studied by circular dichroism (CD) measurements allows us to conclude that the CD within the bands of bound Z is mainly due to the chirality of the first sphere and that the greatest part of 3 is bound in the M-conformation. For Z* we conclude that (S)-1 binds on both binding sites of HSA in the M-conformation, while (R)-1 binds on two different binding sites in opposite conformations. Furthermore we conclude that binding via two nitrogens of the benzodiazepine, i.e. at two ends of the chromophoric system is rather more probable than via ring A. © 1979.