Amino-acids and peptides. Part XXXVI. The synthesis of analogues of bradykinin by the picolyl ester method

Abstract

The picolyl ester method has been used to synthesise the following nine analogues and modifications of bradykinin : [5-β-cyclohexyl-L-alanine]-, [8-β-cyclohexyl-L-alanine]-, [5,8-bis-β-cyclohexyl-L-alanine]-, [1-L-homoarginine,5-β-cyclohexyl-L-alanine]-, [1-L-homoarginine]-, [1-L-valine]-, [1-L-valine,6-L-threonine]-, and [1-L-leucine,6-L-threonine]-bradykinin, and t-butoxycarbonylbradykinin. The first five analogues have, in the tests applied, biological activity similar to that of bradkyinin; the remainder have no significant activity.