820216-53-3

Upstream product

• 820216-31-7 butane-1-sulfonic acid 3-(2-tert-butoxycarbonylamino-propyl)-1H-indol-7-yl ester 
• 244081-38-7 (2R)-7-benzyloxy-3-[2-(tert-butoxycarbonylamino)propyl]-1H-indole 
• 776302-32-0 (R)-3-[2-(tert-butoxycarbonylamino)propyl]-7-hydroxy-1H-indole 
• 776302-69-3 (R)-2-bromo-1-(tert-butyldimethylsilyloxy)-1-(3-nitrophenyl)ethane 
• 820216-60-2 3-[2-bromo-1-(tert-butyl-dimethyl-silanyloxy)-ethyl]-phenylamine 
• 193761-55-6 (R)-2-bromo-1-(3-nitrophenyl)ethan-1-ol 
• 2227-64-7 3'-nitro-2-bromoacetophenone 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 820216-39-5 butane-1-sulfonic acid 3-(2-amino-propyl)-1H-indol-7-yl ester 
• 776302-68-2 (R)-N-{3-[2-bromo-1-(tert-butyldimethylsilyloxy)ethyl]phenyl}(2-thiophene)sulfonamide 

Relevant academic research and scientific papers

Tryptamine-based human β3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring

The synthesis and biological evaluation of a series of tryptamine-based β3-adrenergic receptor (AR) agonists are described. The methanesulfonate 54 exhibited strong agonistic activity and excellent subtype selectivity for the β3-AR. A series of tryptamine-based 2-thiophenesulfonamide derivatives were prepared and their agonistic activity for the β-adrenergic receptors (ARs) was evaluated. Compound 54, containing 7-methanesulfonyloxy tryptamine, was found to be a highly potent β3-AR agonist (EC50 = 0.21 nM, IA = 97%) with excellent selectivity for the β3-AR over the β1- and β2-ARs (210- and 86-fold, respectively).