Chapter 9: Prostaglandin Structure-Activity Relationships

摘要: Publisher Summary Extensive pharmacological evaluation of unique natural products like extremely potent C 20 fatty acids has, however, uncovered a broad spectrum activities, both in animals and man. Despite the demonstration activity, original optimistic predictions clinical utility for prostaglandins have not been realized. The lack selectivity oral efficacy, chemical instability, short duration action materials limited their commercial use to prostaglandin F 2α , (dinoprost tromethamine) as an abortifacient E 2 (dinoprostone) inducer labor. Conclusions concerning analog activity must be accepted with caution unless data several biological assays is presented because inactivity one assay may merely reflection selectivity. This chapter summarizes number useful structure–activity relationships (SAR), derived over past decade. As differs widely changes number, type, stereochemistry oxygenated substituents, it seems reasonable that cyclopentane ring analogs would exhibit different profiles. interesting concept substituting heteroatom carbon (and its pendant oxygen function) has investigated synthesis 8-aza, 9-thia, 10-oxa, 11-oxa, 11-thia, 9, 11-dioxa analogs. Animal studies many modified suggest some superior materials. However, exception 15- ldmethylated little reported therapeutic effects