New quinoline-based caging groups synthesized for photo-regulation of aptamer activity
摘要:
A series of quinoline-based photo-removable protecting groups for photo-regulation of thrombin aptamer (HD1) activity were synthesized with improved caging and uncaging efficiency. Among them, 8-bromo-2-diazomethyl-7-hydroxyquinolinyl (BHQ-diazo, 1) chromophore was found to cage the HD1 with highest caging and restoration efficiency. Moreover, on the basis of the RP-HPLC and SPR analysis, BHQ was demonstrated to regulate HD1s specific affinity to target molecule with 3-fold photolysis sensitivity and about 40% percent higher uncaging efficiency than Bhc (6-bromo-7-hydroxycoumarin-4-ylmethyl) group. It was proposed that the development and use of quinoline derivative may provide a general strategy to photo-regulate oligonucleotide's activity with improved caging and uncaging efficiencies by the convenient non-site-specific caging method. (C) 2010 Elsevier B.V. All rights reserved.
Synthesis of New Cholesterol- and Sugar-Anchored Squaraine Dyes: Further Evidence of How Electronic Factors Influence Dye Formation
摘要:
Synthesis of new quinaldine-based squaraine dyes linked to cellular recognition elements that exhibit near-infrared absorption (> 740 nm) are described. Both product analysis and theoretical calculations substantiate the interesting electronic effects of various substituents in the dye formation reaction. These results are useful in the synthesis of symmetrical and unsymmetrical squaraine dyes that can have potential biological and photodynamic therapeutical applications.
N,N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS USEFUL AS MONOAMINES REUPTAKE INHIBITORS
申请人:Kurimura Muneaki
公开号:US20090088406A1
公开(公告)日:2009-04-02
The present invention provides a pyrrolidine compound of General Formula (1)
or a salt thereof, wherein R
101
and R
102
are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
N-N-SUBSTITUTED 3-AMINOPYRROLIDINE COMPOUNDS USEFUL AS MONOAMINES REUPTAKE INHIBITORS
申请人:KURIMURA Muneaki
公开号:US20120065162A1
公开(公告)日:2012-03-15
The present invention provides a pyrrolidine compound of General Formula (1)
or a salt thereof, wherein R
101
and R
102
are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
N,N-substituted 3-aminopyrrolidine compounds useful as monoamines reuptake inhibitors
申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:US10000450B2
公开(公告)日:2018-06-19
The present invention provides a pyrrolidine compound of General Formula (1)
or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
Synthesis of New Cholesterol- and Sugar-Anchored Squaraine Dyes: Further Evidence of How Electronic Factors Influence Dye Formation
作者:Kuthanapillil Jyothish、Rekha R. Avirah、Danaboyina Ramaiah
DOI:10.1021/ol052639j
日期:2006.1.1
Synthesis of new quinaldine-based squaraine dyes linked to cellular recognition elements that exhibit near-infrared absorption (> 740 nm) are described. Both product analysis and theoretical calculations substantiate the interesting electronic effects of various substituents in the dye formation reaction. These results are useful in the synthesis of symmetrical and unsymmetrical squaraine dyes that can have potential biological and photodynamic therapeutical applications.