Topically active carbonic anhydrase inhibitors. 2. Benzo [b] thiophenesulfonamide derivatives with ocular hypotensive activity

SL Graham, KL Shepard, PS Anderson…

文献索引：Graham, Samuel L.; Shepard, Kenneth L.; Anderson, Paul S.; Baldwin, John J.; Best, Darryl B.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 12 p. 2548 - 2554

全文：HTML全文

被引用次数: 84

摘要

3 5 the initial corneal barrier is a highly lipophilic epithelial cell layer, we felt that the intrinsically more lipophilic benzo [b] thiophenes should be more readily absorbed than the corresponding benzothiazole. This might obviate the need for a lipophilic prodrug strategy (Le., the requirement for the pivaloate ester in l), which was required to achieve suitable activity in the benzothiazole series. 2f However, since the factors governing the drug- ...