Bromobenzofuran-based non-peptide antagonists of angiotensin II: GR138950, a potent antihypertensive agent with high oral bioavailability

…, BC Ross, TI Jack, M Pass, E Tranquillini…

文献索引：Judd; Dowle; Middlemiss; Scopes; Ross; Jack; Pass; Tranquillini; Hobson; Panchal; Stuart; Paton; Hubbard; Hilditch; Drew; Robertson; Clark; Travers; Hunt; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 19 p. 3108 - 3120

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被引用次数: 48

摘要

We have identified GR138950, a potent antagonist of the angiotensin I1 receptor with high oral bioavailability, as our second drug candidate to GR117289. Using GR117289, a compound with moderate bioavailability (20%) in man as a lead, we pursued a strategy aimed at enhancing bioavailability. The strategy was based on SAR established around the diacid GR117289, and from this, it was proposed that a monoacid, in particular a ...