1000289-63-3Relevant academic research and scientific papers
Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors
Axford, Lorraine C.,Agarwal, Piyush K.,Anderson, Kelly H.,Andrau, Laura N.,Atherall, John,Barker, Stephanie,Bennett, James M.,Blair, Michael,Collins, Ian,Czaplewski, Lloyd G.,Davies, David T.,Gannon, Carlie T.,Kumar, Dushyant,Lancett, Paul,Logan, Alastair,Lunniss, Christopher J.,Mitchell, Dale R.,Offermann, Daniel A.,Palmer, James T.,Palmer, Nicholas,Pitt, Gary R.W.,Pommier, Stéphanie,Price, Daniel,Narasinga Rao,Saxena, Rashmi,Shukla, Tarun,Singh, Amit K.,Singh, Mahipal,Srivastava, Anil,Steele, Christopher,Stokes, Neil R.,Thomaides-Brears, Helena B.,Tyndall, Edward M.,Watson, David,Haydon, David J.
, p. 6598 - 6603 (2013)
The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties.
MACROCYCLIC RIP2-KINASE INHIBITORS
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Page/Page column 73, (2021/08/06)
The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
A practical nickel-catalyzed reductive alkylation of amidophenyl bromides
Liu, Xuge,Yang, Zhilin,Li, Ya-Min,Yang, Fan,Feng, Liang,Wang, Nengzhong,Ma, Debiao,Chang, Kwen-Jen,Shen, Yuehai
, p. 9522 - 9529 (2015/03/04)
A modified Weix's reductive coupling for alkylation of amidoaryl bromides based on Ni(COD)2 precatalyst and 2,2′-dipyridyl ligand was developed. This reaction is reliable for amidophenyl bromides and gives yields up to 87%, and is potentially useful in the synthesis of amidophenyl-containing molecules.
Antibacterial Compounds
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, (2013/10/07)
The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
ANTIBACTERIAL COMPOUNDS
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, (2012/04/18)
The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
ANTIBACTERIAL COMPOSITIONS
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, (2008/06/13)
Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1 ; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (-O-), thioether (-S-) or amino (-NR)- link, wherein R is hydrogen, -CN or C1-C3 alkyl; X is -C(=O)NR6-, -S(O)NR6-, -C(=O)O- or -S(=O)O- wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or -( C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
