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参考文献:Synthesis Of Polyfluoro Ketones For Selective Inhibition Of Human Phospholipase A2 Enzymes
标题:Synthesis Of Polyfluoro Ketones For Selective Inhibition Of Human Phospholipase A2 Enzymes
摘要:The Development Of Selective Inhibitors For Individual Pla(2) Enzymes Is Necessary In Order To Target Pla(2)-Specific Signaling Pathways,But It Is Challenging Due To The Observed Promiscuity Of Known Pla(2) Inhibitors. In The Current Work,We Present The Development And Application Of A Variety Of Synthetic Routes To Produce Pentafluoro,Tetrafluoro,And Trifluoro Derivatives Of Activated Carbonyl Groups In Order To Screen For Selective Inhibitors And Characterize The Chemical Properties That Can Lead To Selective Inhibition. Our Results Demonstrate That The Pentafluoroethyl Ketone Functionality Favors Selective Inhibition Of The Gvia Ipla(2),A Very Important Enzyme For Which Specific,Potent,Reversible Inhibitors Are Needed. We Find That 1,1,1,2,2-Pentafluoro-7-Phenyl-Heptan-3-One (Fkgk11) Is A Selective Inhibitor Of Gvia Ipla(2) (X-1(50) = 0.0073). Furthermore,We Conclude That The Introduction Of An Additional Fluorine Atom At The Alpha' Position Of A Trifluoromethyl Ketone Constitutes An Important Strategy For The Development Of New Potent Gvia Ipla(2) Inhibitors.
Doi:10.1021/jm800649Q
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专利信息
专利号:WO-2018047197-A1
优先权日:2016-09-07
标 题 :Site-selective peptides and protein labelling and synthesis of homogenous protein conjugates
发明人:RAI VISHAL; CHILAMARI MAHESHWERREDDY; PURUSHOTTAM LANDA
权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES BHOPAL
摘要:The invention pertains to the method for the site selective modification of peptides and proteins comprising of the activation of the single site (N É› -NH 2 ) of peptides and proteins and the method comprising one of formylation; interception of formylation; alkynylation or amino phosphonation of peptides and proteins.
专利号:US-10808128-B2
优先权日:2018-06-11
标题 :Compounds as fluorescent probes, synthesis and applications thereof
发明人:GULYANI AKASH; RAJA SUFI OASIM; SIVARAMAN GANDHI
权利人:INST FOR STEM CELL BIOLOGY AND REGENERATIVE MEDICINE INSTEM
摘要:The present disclosure relates to chemical dyes useful for staining and imaging of cells. In particular, the disclosure relates to compound of Formula I, method of preparation thereof, and it's use as a fluorescent probe for staining and/or imaging mitochondria in cells, tissues or animals, resulting in a range of applications including, but not limiting, to sensing local ordering or viscosity of mitochondria, tracking mitochondrial mobility, comparing & evaluating mitochondrial function, local ordering, microviscosity and dynamics. Said dyes have additional advantages including, but not limiting, to low toxicity, longer shelf-life, generate little or no reactive species upon long term light irradiation and do not perturb the functionality of the mitochondria in cells compared to prior art dyes.
专利号:US-8558012-B2
优先权日:2009-03-02
标 题:2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative, production method thereof, and production method of monofluoromethyl group-containing compound using the same
发明人:SHIBATA NORIO
权利人:SHIBATA NORIO; NAGOYA INST TECHNOLOGY; TOSOH P TECH INC
摘要:A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.
专利号:US-2025189532-A1
优先权日:2022-03-04
标 题:1,6-diyne compound, its preparation method, and products obtained using 1,6-diyne compound as raw material and their applications
发明人:BAO HONGLI; YE CHANGQING; HUANG RUI; ZHU NENGBO
权利人:FUJIAN INST RES STR MATTER CAS
摘要:A 1,6-diynes compound, its preparation method, and products obtained from 1,6-diynes as raw material and their applications are provided. The compound represented by a general formula (I), and its tautomers, polymorphs, solvates, or salts thereof, n n n n n n n n n n The 1,6-diyne compounds provided have variable structures, are easy to be synthesized, and are suitable for industrial production; they can be used for the synthesis of a class of benzoisoindole dimer compounds and their derivatives, cell imaging, and detecting reactive oxygen species (such as sodium hypochlorite, hydrogen peroxide, ozone, etc.). The 3-arylbenzoisoindole compound provided can be used as an important compound and play an important role in pharmaceuticals or fluorescent materials.
专利号:CN-104086345-B
优先权日:2014-06-24
标题 :A kind of method that platinum nanowire catalyzes the synthesis of amides
专利号:RU-2130011-C1
优先权日:1993-06-16
标题 :Alicyclic compounds, a method of their synthesis, a pharmaceutical composition showing anti-inflammatory activity and a method of treatment of patients with inflammation