86984-32-9Relevant articles and documents
Cell necrosis inhibitor, and preparation method and application thereof
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Paragraph 0553-0555, (2020/01/12)
The invention provides a cell necrosis inhibitor, and a preparation method and application thereof. Particularly, the invention provides an inhibitor for inhibiting cell necrosis and/or human receptorinteracting protein 1 kinase (RIP1). The inhibitor has
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors
Harrison, Justin R.,Brand, Stephen,Smith, Victoria,Robinson, David A.,Thompson, Stephen,Smith, Alasdair,Davies, Kenneth,Mok, Ngai,Torrie, Leah S.,Collie, Iain,Hallyburton, Irene,Norval, Suzanne,Simeons, Frederick R. C.,Stojanovski, Laste,Frearson, Julie A.,Brenk, Ruth,Wyatt, Paul G.,Gilbert, Ian H.,Read, Kevin D.
supporting information, p. 8374 - 8389 (2018/09/25)
Crystallography has guided the hybridization of two series of Trypanosoma brucei N-myristoyltransferase (NMT) inhibitors, leading to a novel highly selective series. The effect of combining the selectivity enhancing elements from two pharmacophores is shown to be additive and has led to compounds that have greater than 1000-fold selectivity for TbNMT vs HsNMT. Further optimization of the hybrid series has identified compounds with significant trypanocidal activity capable of crossing the blood-brain barrier. By using CF-1 mdr1a deficient mice, we were able to demonstrate full cures in vivo in a mouse model of stage 2 African sleeping sickness. This and previous work provides very strong validation for NMT as a drug target for human African trypanosomiasis in both the peripheral and central nervous system stages of disease.
COMPOUNDS AND METHODS USEFUL FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION
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Page/Page column 96, (2009/01/20)
Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.
4-aryl-3-(heteroarylureido)quinoline derivatves
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, (2008/06/13)
Compounds of the formula STR1 and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The comp
Intermediates for making N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT)
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, (2008/06/13)
Compounds of the formula STR1 wherein R21 and R22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula STR2 and the pharmaceutically acceptable salts thereof, wherein Q and R1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
New N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase
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, (2008/06/13)
Compounds of the formula the pharmaceutically acceptable salts thereof, wherein Q and R1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.