Captopril rational drug design

Captopril was announced in 1977 by the Squibb group led by Ondetti and Cushman (95,96), and the history of its design has been extensively reviewed (for example in 72,73, 97-102). Attempts to build metabolic stability into the peptide BPP5a were not successful, nor was a viable nonpeptide lead discovered in the Squibb sample collection (101). Captopril instead is one of the landmark achievements of rational drug design. 

---