350228-61-4Relevant articles and documents
Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer Disease
Pudlo, Marc,Luzet, Vincent,Ismaili, Lhassane,Tomassoli, Isabelle,Iutzeler, Anne,Refouvelet, Bernard
, p. 2496 - 2507 (2014/05/06)
Design, synthesis and evaluation of new acetylcholinesterase inhibitors by combining quinolinecarboxamide to a benzylpiperidine moiety are described. Then, a series of hybrids have been developed by introducing radical scavengers. Molecular modeling was performed and structure activity relationships are discussed. Among the series, most potent compounds show effective AchE inhibitions, high selectivities over butyrylcholinesterase and high radical scavenging activities. On the basis of this work, the ability of quinolone derivatives to serve in the design of N-benzylpiperidine linked multipotent molecules for the treatment of Alzheimer Disease has been established.
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole α1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia
Meyer,Altenbach,Bai,Basha,Carroll,Kerwin Jr.,Lebold,Lee,Pratt,Sippy,Tietje,Wendt,Brune,Buckner,Hancock,Drizin
, p. 1971 - 1985 (2007/10/03)
In search of a uroselective α1A subtype selective antagonist, a novel series of 6-OMe hexahydrobenz[e]isoindoles attached to a bicyclic heterocyclic moiety via a two-carbon linker was synthesized. It was found that in contrast to the previously described series of tricyclic heterocycles,1 this bicyclic series has very specific requirements for the heterocyclic attachments. The most important structural features contributing to the α1A/α1B selectivity of these compounds were identified. In vitro functional assays for the α1 adrenoceptor subtypes were used to further characterize the most selective compounds, and in vivo models of vascular vs prostatic tone were used to assess uroselectivity. Compound 48 showed the highest degree of selectivity in the radioligand binding assays (56-fold), in the in vitro functional tests (80-fold), and for in vivo prostate selectivity (960-fold).
