The isolation and structure determination of the naturally occurring LTB4 receptor antagonist Leucettamine A (1) was recently rep0rted. l Herein we describe the synthesis of this natural product, the preparation of several analogues, and their effectiveness as antagonists of I3H1LTB4 binding to intact human U-937 cells. Total synthesis of Leucettamine A (1) is achieved by a convergent route which takes advantage of the elements of symmetry within ...