Bradykinin chemistry

Freidinger, R.M., Bock, M.G., and Anthony, N.J. (2008) 2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists. Journal of Medicinal Chemistry, 51, 3946-3952. 

Prueksaritanont, T, Detwiler, T.J., Hettrick, L.A., Landis, E.R., Leonard, Y.M., Krueger, J.A., Lewis, S.D., Pettibone, D.J., Freidinger, R.M., and Bock, M.G. (2006) Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin Bj receptor antagonists, journal of Medicinal Chemistry, 49, 1231-1234. 

By any criterion this was an outstanding synthesis. Improvements in the chemistry were described which enabled the nonapeptide sequence of bradykinin to be assembled in four da5rs and isolated, purified, and fully characterized in a further five. The overall yield of highly pure, fully active material was 68%. These results greatly exceeded any which could be achieved by contemporary solution methods and triggered an explosion of activity in solid phase peptide synthesis. 

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