Witiak D T, Kakodkar S V, Johnson T P, Baldwin J R, Rahwan R G
J Med Chem. 1979 Jan;22(1):77-81. doi: 10.1021/jm00187a017.
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.
本文阐述了开发前列腺素F2α受体拮抗剂的基本原理。目标类似物5,6-（二苄氧基）-1-氧代-2-丙基-2-茚丙酸（3）在小鼠回肠上对PGF2α的拮抗作用与对乙酰胆碱和氯化钾的拮抗作用相比，显示出选择性活性，而其他未被苄基取代的2-茚丙酸（1、2、4）活性明显较低且无选择性。结果表明，化合物3可作为进一步药物开发的先导化合物。
