Leukotriene B(3) and B(4) are part of an important class of signaling molecules - the leukotrienes, implicated in the inflammation process. Their pro-inflammatory effects have been widely recognized for almost three decades but it is only recently that their benefit in host defense has begun to be acknowledged. Their use as therapeutic agents is, unfortunately, limited by rapid metabolism. However, over the past 25 years, a number of stable leukotriene B(3) and B(4) analogues have been produced. In this review, we examine their medicinal chemistry and biological evaluation.