126489-69-8Relevant academic research and scientific papers
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors
Wilson, Kenneth J.,Illig, Carl R.,Chen, Jinsheng,Wall, Mark J.,Ballentine, Shelley K.,Desjarlais, Renee L.,Chen, Yanmin,Schubert, Carsten,Donatelli, Robert,Petrounia, Ioanna,Crysler, Carl S.,Molloy, Christopher J.,Chaikin, Margery A.,Manthey, Carl L.,Player, Mark R.,Tomczuk, Bruce E.,Meegalla, Sanath K.
scheme or table, p. 3925 - 3929 (2010/09/03)
During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead ary
Pyrimidines and uses thereof
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, (2008/06/13)
The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design
Chand, Pooran,Babu, Yarlagadda S.,Bantia, Shanta,Chu, Naiming,Cole, L. Brent,Kotian, Pravin L.,Laver, W. Graeme,Montgomery, John A.,Pathak, Ved P.,Petty, Sandra L.,Shrout, David P.,Walsh, David A.,Walsh, Gerald M.
, p. 4030 - 4052 (2007/10/03)
A series of 94 benzoic acid derivatives was synthesized and tested for its ability to inhibit influenza neuraminidase. The enzyme-inhibitor complex structure was determined by X-ray crystallographic analysis for compounds which inhibited the enzyme. The most potent compound tested in vitro, 5 (4- (acetylamino)-3-guanidinobenzoic acid), had an IC50 = 2.5 x 10-6 M against N9 neuraminidase. Compound 5 was oriented in the active site of the neuraminidase in a manner that was not predicted from the reported active site binding of GANA (4) with neuraminidase. In a mouse model of influenza, 5 did not protect the mice from weight loss due to the influenza virus when dosed intranasally.
