463297-75-8Relevant academic research and scientific papers
A divergent synthesis of minor groove binders with tail group variation
Breen, David,Kennedy, Alan R.,Suckling, Colin J.
experimental part, p. 178 - 186 (2009/04/07)
A new synthesis of polyamide minor groove binders in which diversity is introduced by the nucleophilic substitution of a 2-sulfido-1,3,2- diazaphospholidinyloxy substituent by volatile secondary amine nucleophiles is described. Such a method has potential
NOVEL MINOR GROOVE BINDERS
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Page/Page column 72, (2008/06/13)
There is provided compounds of formula (I), wherein R1, R11, R12, Qa, X, Qb, Qc, A and D have meanings given in the description, or a pharmaceutically acceptable salt or solvate thereof, which compound, salt or solvate binds to the minor groove of DNA.
Antimicrobial lexitropsins containing amide, amidine, and alkene linking groups
Anthony, Nahoum G.,Breen, David,Clarke, Joanna,Donoghue, Gavin,Drummond, Allan J.,Ellis, Elizabeth M.,Gemmell, Curtis G.,Helesbeux, Jean-Jacques,Hunter, Iain S.,Khalaf, Abedawn I.,Mackay, Simon P.,Parkinson, John A.,Suckling, Colin J.,Waigh, Roger D.
, p. 6116 - 6125 (2008/09/16)
The synthesis and properties of 80 short minor groove binders related to distamycin and the thiazotropsins are described. The design of the compounds was principally predicated upon increased affinity arising from hydrophobic interactions between minor groove binders and DNA. The introduction of hydrophobic aromatic head groups, including quinolyl and benzoyl derivatives, and of alkenes as linkers led to several strongly active antibacterial compounds with MIC for Staphylococcus aureus, both methicillin-sensitive and -resistant strains, in the range of 0.1-5 μg mL-1, which is comparable to many established antibacterial agents. Antifungal activity was also found in the range of 20-50 μg mL-1 MIC against Aspergillus niger and Candida albicans, again comparable with established antifungal drugs. A quinoline derivative was found to protect mice against S. aureus infection for a period of up to six days after a single intraperitoneal dose of 40 mg kg-1.
6-(2-Phenylethyl)nicotine: A novel nicotinic cholinergic receptor ligand
Ramunno, Anna,Dukat, Malgorzata,Lee, Mase,Young, Richard,El-Zahabi, Mohamed,Damaj, M. Imad,Martin, Billy,Glennon, Richard A.
, p. 3237 - 3240 (2007/10/03)
6-(2-Phenylethyl)nicotine (1b; Ki = 15 nM) was unexpectedly found to bind at α4β2 nicotinic cholinergic (nACh) receptors. Although this compound failed to produce nicotine-like agonist action in several functional assays, 1b antagonized the ant
Synthesis of (E)-5-(2-arylvinyl)-2-(hetero)arylpyridines, (E)-2-(2-arylvinyl)-5-methoxycarbonylpyridines and (E,E)-2,5-bis(2-arylvinyl)pyridines as polarity and pH probes
Van der Eycken, Erik,Jidong, Zhang,Kilonda, Amuri,Compernolle, Frans,Toppet, Suzanne,Hoornaert, Georges,Van der Auweraer, Mark,Jackers, Carine,Verbouwe, Wouter,De Schryver, Frans C.
, p. 928 - 937 (2007/10/03)
In this report we describe the synthesis photophysical properties (E)-5-(2-arylvinyl)-2-(hetero)-and of various arylpyridines 7a-f, (E)-2-(2-arylvinyl)-5-methoxycarbonylpyridines 14a,b and (E,E)-2,5-bis(2-arylvinyl)pyridines 13a,b. The fluorescence spectr
Esters of substituted nicotinic acids
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, (2008/06/13)
Novel derivatives of nicotinic acid possessing vasomotor properties.
