114652-98-1Relevant academic research and scientific papers
Rapid Generation of Complex Molecular Architectures by a Catalytic Enantioselective Dearomatization Strategy
Williamson, Alice E.,Ngouansavanh, Tifelle,Pace, Robert D. M.,Allen, Anna E.,Cuthbertson, James D.,Gaunt, Matthew J.
, p. 116 - 120 (2016)
A catalytic enantioselective dearomatization strategy can be used to convert readily assembled phenols into complex polycyclic architectures. By combining oxidative dearomatization of phenols bearing a pendent nucleophile with enantioselective secondary a
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors
Aoyama, Yasunori,Uenaka, Masaaki,Konoike, Toshiro,Iso, Yasuyoshi,Nishitani, Yasuhiro,Kanda, Akiko,Naya, Noriyuki,Nakajima, Masatoshi
, p. 2397 - 2401 (2007/10/03)
1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes. (C) 2000 Elsevier Science Ltd.
Soft Drugs. 7. Soft β-Blockers for Systemic and Ophthalmic Use
Bodor, Nicholas,El-Koussi, Alaaeldin A.,Kano, Masanobu,Khalifa, Mohamed M.
, p. 1651 - 1656 (2007/10/02)
The "inactive metabolite approach" used to design a series of "soft" drugs derived from the acidic metabolite of metoprolol.Pharmacokinetic and pharmacodynamic properties of these novel "soft" β-adrenoceptor antagonists were determined: half-lives in human blood ranged from 5 to 754 min.The rates of in vivo disappearance of representative slow, medium, and fast hydrolyzing esters were determined in rats.In each case rapid and quantitative conversion to the corresponding free acid was observed.This suggests a facile, one-step degradation to the predicted major metabolite.The compounds were tested for their ability to decrease intraocular pressure in a rabbit model.Five of the new compounds exerted an ocular hypotensive action comparable to or greater than of the reference compound, timolol maleate, and with a prolonged duration of action in some cases.In contrast the new compounds showed reduced and shorter duration systemic activity.The adamantylethyl ester emerges as a potentially effective antiglaucoma agent with significantly improved site-specific activity.
