Salerno Loredana, Modica Maria N, Romeo Giuseppe, Pittala Valeria, Cagnotto Alfredo, Siracusa Maria A
Dipartimento di Scienze del Farmaco, Universita degli Studi di Catania, Viale A. Doria, 6, 95125 - Catania, Italy.
Med Chem. 2015;11(2):109-17. doi: 10.2174/1573406410666140917160653.
The interest of researchers for ligands of the endothelin receptors ETA and ETB is due to their extensive therapeutic potential. In particular, receptor antagonists are useful in a number of diseases such as pulmonary hypertension, acute myocardial infarction, congestive heart failure, renal failure, and atherosclerosis. In the context of our research program aimed to the development of new endothelin receptor ligands, in this paper we describe the synthesis and structure- activity relationships of a new series of 1,3,5-substituted pyrrole-2-carboxylic acid derivatives 27-40 possessing the structural features for ET receptors binding. New synthesized compounds were tested on ETA and ETB receptors stably expressed in CHO cells and some of them showed interesting affinity and selectivity towards ETA receptors.
研究人员对内皮素受体ETA和ETB的配体感兴趣，是因为它们具有广泛的治疗潜力。特别是，受体拮抗剂在多种疾病中都很有用，如肺动脉高压、急性心肌梗死、充血性心力衰竭、肾衰竭和动脉粥样硬化。在我们旨在开发新的内皮素受体配体的研究项目背景下，本文描述了一系列具有ET受体结合结构特征的新型1,3,5-取代吡咯-2-羧酸衍生物27-40的合成及其构效关系。新合成的化合物在CHO细胞中稳定表达的ETA和ETB受体上进行了测试，其中一些对ETA受体表现出有趣的亲和力和选择性。
