Chapter 7. Pulmonary and Antiallergy Agents

Abstract

Publisher Summary Research on arachidonic acid and its various metabolites have proceded at a brisk pace. Cyclooxygenase and lipoxygenase products have been the matter of interest. However, the clinical benefit of this type of agent remains unclear until clinical data appear on the agents affecting arachidonic acid metabolites, whether inhibiting the synthesis of leukotrienes, blocking release or effects of slow reacting substance (SRS), or inhibiting lipoxygenase products. Several significant researches describe new synthetic preparations of leukotrienes. A stereospecific synthesis of leukotrienes from 2-deoxy- d -ribose has been described in the chapter and LTC 4 , LTD 4 , and LTE4 have been prepared from 5-HPETE by a stereoselective, biomimetic route. Eight synthetic isomers of LTD 4 have been synthesized and compared. Only the 5S, 6R, 7, 9-trans, 11, and 14-cis isomer are found identical to the biologically-generated guinea pig LTD 4 in all respects. In another study, involving the analogs of LTC 4 and LTD 4 , it is found that the 5-OH and carboxyl groups are essential for SRS activity but variation of the peptide moiety only partially decreased the activity. Sulfones of LTC 4 , LTD 4 , and LTE 4 have been prepared from the corresponding LTs. They are biologically similar to the LTs with about half the potency.