Bundy G L, Morton D R, Peterson D C, Nishizawa E E, Miller W L
J Med Chem. 1983 Jun;26(6):790-9. doi: 10.1021/jm00360a003.
Several prostaglandin D (PGD) analogues have been synthesized, incorporating the following variations: (a) varying degrees of side-chain unsaturation, (b) C-9 hydroxy removed or in the unnatural 9 beta configuration, (c) metabolically stabilized analogues (e.g., 15-methyl, 16,16-dimethyl, 17-phenyl, etc.), and (d) delta 12 isomers resulting from decomposition of PGD2. With regard to their ability to inhibit adenosine diphosphate (ADP) induced human platelet aggregation: (a) PGD3 greater than or equal to PGD2 greater than PGD1 greater than 13,14-dihydro-PGD1, (b) the 9 beta- and 9-deoxy-PGD2 analogues are more potent than PGD2, (c) metabolically stabilized analogues with bulky substituents at or near C-15 have substantially reduced antiaggregatory activity relative to PGD2 and (d) the delta 12 isomers of PGD2 are much less active than PGD2.
已合成了几种前列腺素D（PGD）类似物，包含以下几种变体：（a）不同程度的侧链不饱和；（b）C-9位羟基被去除或呈非天然的9β构型；（c）代谢稳定的类似物（如15-甲基、16,16-二甲基、17-苯基等）；以及（d）由PGD2分解产生的Δ12异构体。关于它们抑制二磷酸腺苷（ADP）诱导的人血小板聚集的能力：（a）PGD3≥PGD2＞PGD1＞13,14-二氢-PGD1；（b）9β-和9-脱氧-PGD2类似物比PGD2更有效；（c）在C-15位或其附近带有庞大取代基的代谢稳定类似物相对于PGD2具有显著降低的抗聚集活性；以及（d）PGD2的Δ12异构体的活性远低于PGD2。
