CAS: 41213-04-1; 1-[4-Chloro-3-(Trifluoromethyl)Phenyl]Piperazine

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CAS号110-85-0 哌嗪 | CAS号445-01-2 5-溴-2-氯三氟甲苯 | CAS号91703-25-2 5-[4-[4-chloro-...

4-氯-3-(三氟甲基)苯硼酸置于copper Diacetate,三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 1.08H,反应生成 氯三氟甲基苯基哌嗪
参考文献:4-(3-Chloro-5-(Trifluoromethyl)Pyridin-2-yl)-N-(4-Methoxypyridin-2-yl)Piperazine-1-Carbothioamide (Ml267),A Potent Inhibitor Of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary Metabolism And Thwarts Bacterial Growth
标题:4-(3-Chloro-5-(Trifluoromethyl)Pyridin-2-yl)-N-(4-Methoxypyridin-2-yl)Piperazine-1-Carbothioamide (Ml267),A Potent Inhibitor Of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary Metabolism And Thwarts Bacterial Growth
摘要:4'-Phosphopantetheinyl Transferases (Pptases) Catalyze A Post-Translational Modification Essential To Bacterial Cell Viability And Virulence. We Present The Discovery And Medicinal Chemistry Optimization Of 2-Pyridinyl-N-(4-Aryl)-Piperazine-1-Carbothioamides,Which Exhibit Submicromolar Inhibition Of Bacterial Sfp-Pptase With No Activity Toward The Human Orthologue. Moreover,Compounds Within This Class Possess Antibacterial Activity In The Absence Of A Rapid Cytotoxic Response In Human Cells. An Advanced Analogue Of This Series,Ml267 (55),Was Found To Attenuate Production Of An Sfp-Pptase-Dependent Metabolite When Applied To Bacillus Subtilis At Sublethal Doses. Additional Testing Revealed Antibacterial Activity Against Methicillin-Resistant Staphylococcus Aureus,And Chemical Genetic Studies Implicated Efflux As A Mechanism For Resistance In Escherichia Coli. Additionally,We Highlight The In Vitro Absorption,Distribution,Metabolism; And Excretion And In Vivo Pharmacokinetic Profiles Of Compound 55 To Further Demonstrate The Potential Utility Of This Small-Molecule Inhibitor.
DOI:10.1021/jm401752P

专利信息

专利号:US-2005019747-A1
优先权日:2002-08-07
标 题 :Nanoliter-scale synthesis of arrayed biomaterials and screening thereof
发明人：ANDERSON DANIEL G; LEVENBERG SHULAMIT; LANGER ROBERT S
摘要:A method of screening cell-polymer interactions. The method includes depositing monomers as a plurality of discrete elements on a substrate, causing the deposited monomers to polymerize, thereby creating an array of discrete polymer elements on the substrate, incubating the substrate in a cell-containing culture medium, and characterizing a predetermined cell behavior on each polymer element.

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

专利号:CA-2539670-A1
优先权日:2003-09-15
标 题:Nanoliter-scale synthesis of arrayed biomaterials and screening thereof

专利号:WO-2005028619-A2
优先权日:2003-09-15
标题:Nanoliter-scale synthesis of arrayed biomaterials and screening thereof

专利号:US-9676721-B2
优先权日:2010-09-03
标题 :Compounds and compositions for the inhibition of NAMPT
发明人：BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.

专利号:US-9555039-B2
优先权日:2011-05-09
标题:Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT)
发明人：BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)