225240-71-1Relevant articles and documents
FUSED TRICYCLIC BENZIMIDAZOLES DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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, (2015/06/25)
A series of tricyclic benzimidazole derivatives, in particular dihydro-1H- imidazo [1,2-a]benzimidazo le, dihydro-1H-pyrrolo [1,2-a]benzimidazo le, dihydro-1H- pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
FUSED TRICYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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Page/Page column 114, (2015/06/25)
A series of substituted fused tricyclic imidazole derivatives, in particular dihydro- 1H-pyrano[4',3':4,5]imidazo[1,2-a]pyridine, 1,2,3,4-tetrahydroimidazo[1,2-a:5,4- c']dipyridine, dihydro-1H-pyrano[3',4':4,5]imidazo[1,2-a]pyridine and tetrahydro-6H- cyc
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 (2014/01/06)
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.