340023-04-3Relevant articles and documents
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
, p. 609 - 614 (2014)
Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists
Lu, Zhonghui,Duan, James J.-W.,Xiao, Haiyun,Neels,Wu, Dauh-Rurng,Weigelt, Carolyn A.,Sack, John S.,Khan,Ruzanov, Max,An, Yongmi,Yarde, Melissa,Karmakar, Ananta,Vishwakrishnan, Sureshbabu,Baratam, Venkata,Shankarappa, Harisha,Vanteru, Sridhar,Babu, Venkatesh,Basha, Mushkin,Kumar Gupta, Arun,Kumaravel, Selvakumar,Mathur, Arvind,Zhao, Qihong,Salter-Cid, Luisa M.,Carter, Percy H.,Murali Dhar
, p. 2265 - 2269 (2019/07/03)
An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that the cyclohexane carboxylic acid group of compound 2 plays a significant role in RORγt binding, forming four hydrog
BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 71-72, (2013/03/26)
Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
Adenosine receptor antagonists and methods of making and using the same
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Page/Page column 37, (2008/06/13)
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1receptor. Adenosine A1antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: ?and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.