741703-34-4Relevant academic research and scientific papers
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists
Gavai, Ashvinikumar V.,Vaz, Roy J.,Mikkilineni, Amarendra B.,Roberge, Jacques Y.,Liu, Yalei,Lawrence, R. Michael,Corte, James R.,Yang, Wu,Bednarz, Mark,Dickson Jr., John K.,Ma, Zhengping,Seethala, Ramakrishna,Feyen, Jean H. M.
, p. 5478 - 5482 (2005)
A 3D quantitative structure-activity relationship study for inhibition of calcium-sensing receptor in the aryloxypropanolamine series predicted that these molecules adopt a U-shaped conformation with pi-stacking between the two aromatic rings. This hypoth
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase
Ronkin, Steven M.,Badia, Michael,Bellon, Steve,Grillot, Anne-Laure,Gross, Christian H.,Grossman, Trudy H.,Mani, Nagraj,Parsons, Jonathan D.,Stamos, Dean,Trudeau, Martin,Wei, Yunyi,Charifson, Paul S.
scheme or table, p. 2828 - 2831 (2010/08/19)
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphlococcus aureus GyrB.
