2-Indanpropionic acids: structural leads for prostaglandin F2alpha antagonist development.
A rationale is presented for the development of prostaglandin F2alpha receptor antagonists. The target analogue, 5,6-(dibenzyloxy)-1-oxo-2-propyl-2-indanpropionic acid (3), was shown to have selective activity for antagonism of PGF2alpha when compared to the antagonism of acetylcholine and KCl on the mouse ileum, whereas other 2-indanpropionic acids (1, 2, 4), not substituted with benzyl functions, were considerably less active and nonselective. The results suggest that 3 may serve as a lead compound for further drug development.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D007192:Indenes / Q000138:chemical synthesis*; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011189:Potassium Chloride / Q000037:antagonists & inhibitors; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology; D011460:Prostaglandins F / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007189:Indans; D007192:Indenes; D011422:Propionates; D011460:Prostaglandins F; D011189:Potassium Chloride; D000109:Acetylcholine