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Synthetic strategy and structure–activity relationship (SAR) studies of 3-(5′-hydroxymethyl-2′-furyl)-1-benzyl indazole (YC-1, Lificiguat): a review
RSC Advances ( IF 3.9 ) Pub Date : 2021-12-20 , DOI: 10.1039/d1ra08120a Ko-Hua Yu, Hsin-Yi Hung
RSC Advances ( IF 3.9 ) Pub Date : 2021-12-20 , DOI: 10.1039/d1ra08120a Ko-Hua Yu, Hsin-Yi Hung
Since 1994, YC-1 (Lificiguat, 3-(5′-hydroxymethyl-2′-furyl)-1-benzylindazole) has been synthesized, and many targets for special bioactivities have been explored, such as stimulation of platelet-soluble guanylate cyclase, indirect elevation of platelet cGMP levels, and inhibition of hypoxia-inducible factor-1 (HIF-1) and NF-κB. Recently, Riociguat®, the first soluble guanylate cyclase (sGC) stimulator drug used to treat pulmonary hypertension and pulmonary arterial hypertension, was derived from the YC-1 structure. In this review, we aim to highlight the synthesis and structure–activity relationships in the development of YC-1 analogs and their possible indications.
中文翻译:
3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole (YC-1, Lificiguat) 的合成策略和构效关系 (SAR) 研究:综述
自 1994 年以来,YC-1(Lificiguat,3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole)已被合成,并探索了许多特殊生物活性的靶点,例如刺激血小板可溶性鸟苷酸环化酶,间接升高血小板 cGMP 水平,抑制缺氧诱导因子-1 (HIF-1) 和 NF-κB。最近,第一个用于治疗肺动脉高压和肺动脉高压的可溶性鸟苷酸环化酶 (sGC) 刺激剂药物 Riociguat® 衍生自 YC-1 结构。在这篇综述中,我们旨在强调 YC-1 类似物开发过程中的合成和构效关系及其可能的适应症。
更新日期:2021-12-20
中文翻译:
3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole (YC-1, Lificiguat) 的合成策略和构效关系 (SAR) 研究:综述
自 1994 年以来,YC-1(Lificiguat,3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole)已被合成,并探索了许多特殊生物活性的靶点,例如刺激血小板可溶性鸟苷酸环化酶,间接升高血小板 cGMP 水平,抑制缺氧诱导因子-1 (HIF-1) 和 NF-κB。最近,第一个用于治疗肺动脉高压和肺动脉高压的可溶性鸟苷酸环化酶 (sGC) 刺激剂药物 Riociguat® 衍生自 YC-1 结构。在这篇综述中,我们旨在强调 YC-1 类似物开发过程中的合成和构效关系及其可能的适应症。