183742-33-8Relevant articles and documents
NOVEL IN-VIVO PROBE FOR REAL TIME LONGITUDINAL MONITORING OF INDUCIBLE NITRIC-OXIDE SYNTHASE IN LIVING CELLS AND ANIMALS
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, (2018/06/06)
The present disclosure relates to an in vivo fluorescent or radioactive probe represented by a compound of formula I which is capable of longitudinal imaging of inducible nitric oxide synthase (iNOS) expression in living cells and living animals on a real time basis. The probe of the present disclosure can exhibit specific and high affinity binding to the iNOS enzyme with reduced enzyme inhibitory property and also enables longitudinal monitoring of iNOS expression along with its activity or NO production in a same experimental subject throughout the progression of a physiological or disease process without employing separate subjects as controls and experimental. The present disclosure further provides a rapid and inexpensive real time method for visualizing iNOS expression and its activity in living cells and living animals precisely, conveniently and reversibly along with simultaneous in vivo imaging of its catalytic product, nitric oxide (NO) in live physiological settings.
Benzodiazepine and Pyridodiazepine Derivatives
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, (2011/12/12)
The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors
Davey, David D.,Adler, Marc,Arnaiz, Damian,Eagen, Keith,Erickson, Shawn,Guilford, William,Kenrick, Margaret,Morrissey, Michael M.,Ohlmeyer, Mike,Pan, Gonghua,Paradkar, Vidyadhar M.,Parkinson, John,Polokoff, Mark,Saionz, Kurt,Santos, Cecile,Subramanyam, Babu,Vergona, Ron,Wei, Robert G.,Whitlow, Marc,Ye, Bin,Zhao, Zuchun,Devlin, James J.,Phillips, Gary
, p. 1146 - 1157 (2007/10/03)
By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit the dimerization of iNOS monomers, thus preventing the formation of the dimeric, active form of the enzyme. Optimization led to the selection of the potent, selective, and orally available iNOS dimerization inhibitor, 21b, which significantly ameliorated adjuvant-induced arthritis in a rat model. Analysis of the crystal structure of the 21b-iNOS monomer complex provided a rationalization for both the SAR and the mechanism by which 21b blocks the formation of the protein-protein interaction present in the dimeric form of iNOS.
QUINOLINE DERIVATIVES AS ANTIBACTERIALS
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Page 15, (2010/02/06)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof: corresponding novel medicaments, pharmaceutical compositions and/or methods of
N-heterocyclic derivatives as NOS inhibitors
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, (2008/06/13)
N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.