165803-97-4

Upstream product

• 272130-79-7 3-[2-(tert-butyl-dimethyl-silanyloxy)-ethyl]-4-ethyl-benzoic acid methyl ester 
• 272130-77-5 methyl 3-(2-tert-butyldimethylsilyloxyethyl)-4-vinylbenzoate 
• 272130-76-4 methyl 3-(2-tert-butyldimethylsilyloxy)-4-hydroxybenzoate 
• 99-76-3 methyl 4-hydroxylbenzoate 
• 53596-60-4 methyl 3-allyl-4-hydroxybenzoate 
• 272130-81-1 4-ethyl-3-(2-hydroxy-ethyl)-benzoic acid methyl ester 

Downstream Products

• 1026862-04-3 4-ethyl-3-[2-(8-oxo-7,8-dihydro-6H-imidazo[4,5-d][1,3]diazepin-3-yl)-ethyl]-benzoic acid methyl ester 
• 165801-70-7 4-ethyl-3-[2-(8-hydroxy-7,8-dihydro-6H-imidazo[4,5-d][1,3]diazepin-3-yl)-ethyl]-benzoic acid methyl ester 

Relevant academic research and scientific papers

AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues

N3-Substituted coformycin aglycon analogues with improved AMP deaminase (AMPDA) inhibitory potency are described. Replacement of the 5-carboxypentyl substituent in the lead AMPDA inhibitor 3-(5-carboxypentyl)-3,6,7,8- tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (2) described in the previous article with various carboxyarylalkyl groups resulted in compounds with 10- 100-fold improved AMPDA inhibitory potencies. The optimal N3 substituent had m-carboxyphenyl with a two-carbon alkyl tether. For example, 3-[2-(3-carboxy- 5-ethylphenyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (43g) inhibited human AMPDA with a K(i) = 0.06 μM. The compounds within the series also exhibited > 1000-fold specificity for AMPDA relative to adenosine deaminase.

INHIBITORS OF ADENOSINE MONOPHOSPHATE DEAMINASE

Novel diazepine derivatives which selectively inhibit adenosine monophosphate deaminase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine