COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
申请人:Johansen Lisa M.
公开号:US20100009970A1
公开(公告)日:2010-01-14
The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.
Synthesis and Central Dopaminergic Effects of N-(4,6-Dimethyl-2-pyridinyl)benzamides
作者:Saïd Bouhayat、Sylvie Piessard、Guillaume Le Baut、Louis Sparfel、Jean-Yves Petit、François Piriou、Lucien Welin
DOI:10.1021/jm50001a004
日期:1985.5
N-(4,6-Dimethyl-2-pyridinyl)benzamides 1-24 and the corresponding tertiary derivatives 29-33 were synthesized and studied for possible dopamine-inhibitory properties by testing their effect on motility of naive and reserpinized mice. Unlike the orthopramides, they failed to show any antidopaminergic properties, but some of the secondary derivatives showed instead effects of postsynaptic dopaminergic
Non-acidic antiinflammatory compounds II. Synthesis and activity of 6-amino-2,4-lutidine derivatives
作者:J ROBERT、S ROBERTPIESSARD、M DUFLOS、G LEBAUT、E KHETTAB、N GRIMAUD、J PETIT、L WELIN
DOI:10.1016/0223-5234(94)90107-4
日期:——
Benzamides I, phenylalkanamides II and cinnamamides III are structurally related to the antiinflammatory N-(4,6-dimethylpyridin-2-yl)benzamide 1. These were synthesized and the transformation of the 2-aminopyridine nucleus of benzamides I into a 2-imino-1,2-dihydropyridine structure (compounds IV) was also carried out. Of the 49 new derivatives, the 3-fluorobenzamide 9 was the most potent in the oral treatment of carrageenen-induced peripheral edema; IC50 = 12.2 mg.kg(-1). It was 3 times as active as benzamide 1, but the latter nevertheless had a better therapeutic index (LD(50)/IC50) of 52 against 23. Benzamide 1, a non-acidic antiinflammatory compound devoid of any blocking activity on cyclooxygenase, markedly reduces the production of reactive oxygen species in rat peritoneal macrophages. This compound probably acts at the membrane, perhaps by interference with transmembrane events.
Synthesis and characterization of N-(2-pyridyl)benzamide-based nickel complexes and their activity for ethylene oligomerization
作者:Wen-Hua Sun、Wen Zhang、Tielong Gao、Xiubo Tang、Liyi Chen、Yan Li、Xianglin Jin
DOI:10.1016/j.jorganchem.2003.12.022
日期:2004.3
A series of N-(2-pyridyl)benzamides (1)-(11) and their nickel complexes, [N-(2-pyridyl)benzamide]dinickel(II) di-mu-bromide dibromide (12)-(16) and (aryl)[N-(2-pyridyl)benzamido](triphenylphosphine)nickel(II) (17)-(24), were synthesized and characterized. The single-crystal X-ray analysis revealed that 12 and 14 are binuclear nickel complexes bridged by bromine atoms and each nickel atom adopts a distorted trigonal bipyramidal geometry. The key feature of the complexes 17, 19 and 23 is each has a six-membered nickel chelate ring including a deprotonated secondary nitrogen atom and an O-donor atom. The nickel complexes show moderate to high catalytic activity for ethylene oligomerization with methylaluminoxane (MAO) as cocatalyst. The activity of 12-16/MAO systems is up to 3.3 x 10(4) g mol(-1) h(-1) whereas for 17-24/MAO systems it is up to 4.94 x 10(5) g mol(-1) atm(-1) h(-1). The influence of Al/Ni molar ratio, reaction temperature, reaction period and PPh3/Ni molar ratio on catalytic activity was investigated. (C) 2004 Elsevier B.V. All rights reserved.