N-PHENYL ANTHRANILIC ACID DERIVATIVES AND USES THEREOF
申请人:Attali Bernard
公开号:US20100137296A1
公开(公告)日:2010-06-03
Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.
作者:Emilia Păunescu、Sarah McArthur、Mylène Soudani、Rosario Scopelliti、Paul J. Dyson
DOI:10.1021/acs.inorgchem.5b02690
日期:2016.2.15
we prepared a series of organometallic ruthenium(II)- and osmium(II)-p-cymene complexes modified with the nonsteroidal anti-inflammatory drugs (NSAIDs) indomethacin and diclofenac. The NSAIDs are attached to the organometallic moieties via monodentate (pyridine/phosphine) or bidentate (bipyridine) ligands, affording piano-stool Ru(II) and Os(II) arene complexes of general formula [M(η6-p-cymene)Cl2(N)]
在某些情况下,与单独的对应物相比,已显示将基于金属的药物与共价连接的靶向有机药物结合的化合物显示出优异的抗癌特性。在此框架内,我们制备了一系列用非甾体抗炎药吲哚美辛和双氯芬酸修饰的有机金属钌(II)-和(II)-对-肉桂烯配合物。在NSAIDS中通过单齿(吡啶/膦)二齿或(联吡啶)的配体附着到该有机金属基团,得到钢琴凳的Ru(II)和Os(II)芳烃通式[M的配合物(η 6 - p -cymene) Cl 2(N)],其中N是基于吡啶的配体,2-(2-(1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1 H-吲哚-3-基)乙酰氧基)乙基-3-(吡啶-3-基)丙酸甲酯}或2-(2-(2 - ((2,6-二氯苯基)氨基)苯基)乙酰氧基)乙基-3-(吡啶-3-基)丙酸甲酯},[M(η 6 - p - cymene)Cl 2(P)],其中P是膦配体,2-(2-(1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1