Author/Authors :
Edward K. Dziadulewicz، نويسنده , , Michael C. Brown، نويسنده , , Andrew R. Dunstan، نويسنده , , Wai Lee، نويسنده , , Najeeb B. Said، نويسنده , , Peter J. Garratt، نويسنده ,
Abstract :
The Bradykinin B2 receptor antagonist HOE 140 (D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg) has been used as a template for the de novo design and synthesis of a small number of non-peptide lead compounds based on the 1,4-benzodiazepin-2-one framework. Two of the compounds have been found to exhibit moderate Ki values of 8.9 and 9.2 μM at the human Bradykinin B2 receptor.