19248-13-6Relevant academic research and scientific papers
Discovery of small molecule antagonists of TRPV1
Rami, Harshad K.,Thompson, Mervyn,Wyman, Paul,Jerman, Jeffrey C.,Egerton, Julie,Brough, Stephen,Stevens, Alexander J.,Randall, Andrew D.,Smart, Darren,Gunthorpe, Martin J.,Davis, John B.
, p. 3631 - 3634 (2007/10/03)
Small molecule antagonists of the vanilloid receptor 1 (TRPV1, also known as VR1) are disclosed. Ureas such as 5 (SB-452533) were used to explore the structure activity relationship with several potent analogues identified. Pharmacological studies using electrophysiological and FLIPR Ca2+ based assays showed compound 5 was an antagonist versus capsaicin, noxious heat and acid mediated activation of TRPV1. Study of a quaternary salt of 5 supports a mode of action in which compounds from this series cause inhibition via an extracellularly accessible binding site on the TRPV1 receptor.
2-aminobenzoxazole derivatives and combinatorial libraries thereof
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, (2008/06/13)
The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: wherein R1 to R4 and Z have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminobenzoxazole derivative compounds.
Nucleophilic Ring Opening of 2-Oxazolines with Amines: A Convenient Synthesis for Unsymmetrically Substituted Ethylenediamines
Fazio, Michael J.
, p. 4889 - 4893 (2007/10/02)
The reaction of 2-alkyl-2-oxazolines with alkyl- and arylamines was investigated.The acid-catalyzed nucleophilic ring opening of the 2-oxazolines yields N-(2-aminoethyl)carboxamides in good to excellent yields with secondary amines and hindered primary amines.The N-(2-aminoethyl)carboxamides were hydrolyzed under acidic or basic conditions to selectively yield unsymmetrically substituted ethylenediamines.
