1171124-68-7Relevant articles and documents
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
Bamborough, Paul,Chung, Chun-Wa,Furze, Rebecca C.,Grandi, Paola,Michon, Anne-Marie,Sheppard, Robert J.,Barnett, Heather,Diallo, Hawa,Dixon, David P.,Douault, Clement,Jones, Emma J.,Karamshi, Bhumika,Mitchell, Darren J.,Prinjha, Rab K.,Rau, Christina,Watson, Robert J.,Werner, Thilo,Demont, Emmanuel H.
, p. 6151 - 6178 (2015)
ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor outcomes in a number of different cancer types. To date, no potent and selective inhibitors of the bromodomain have been reported. This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.
HYDROXYALKYL THIADIAZOLE DERIVATIVES
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, (2017/05/07)
Problem to be solved. There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. Solution to the Problem. As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit, possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.
IMIDAZOLE CARBONYL COMPOUND
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Page/Page column 82, (2010/09/17)
To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.