593269-10-4

Upstream product

• 270260-72-5 tert-butyl (3-thioureidopropyl)carbamate 
• 82102-48-5 3-bromo-1-o-methylphenylpropane-1,2-dione 

Downstream Products

• 749846-46-6 [2-(3-amino-propylamino)-thiazol-4-yl]-o-tolyl-methanone 
• 593270-41-8 [2-(3-Amino-propylamino)-thiazol-4-yl]-o-tolyl-methanone hydrochloride 

Relevant academic research and scientific papers

Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor

Sets of isomeric thiazole derivatives 1 and 2 have been synthesised in a parallel iterative solution-phase synthesis approach guided by the SAR analysis derived from biological results and computer-aided design and analysis. This synergistic and streamlined working procedure led to highly active isomeric NPY5 receptor ligands. However, a 10-fold difference at least in their respective binding affinities was consistently found for all isomeric pairs 1 and 2. The analysis of conformational differences due to heteroatom interactions in 1 and 2 revealed a favourable C=O...S interaction in 1, whereas thiazoles 2 showed a repulsive C=O...N interaction.

THIAZOLE DERIVATIVES

Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.