146533-38-2

Upstream product

• 93-40-3 (3,4-Dimethoxyphenyl)acetic acid 
• 896-90-2 2-(3,4-dimethoxyphenyl)malonic acid diethyl ester 
• 98-64-6 4-Chlorobenzenesulfonamide 
• 146533-44-0 5-(3,4-dimethoxyphenyl)-4,6(1H,5H)-pyrimidinedione 
• 18066-68-7 ethyl 3,4-dimethoxyphenylacetate 
• 926008-52-8 5-(3,4-dimethoxyphenyl)pyrimidine-4,6-diol 

Downstream Products

• 926008-72-2 {4-[6-chloro-5-(3,4-dimethoxyphenyl)pyrimidin-4-ylethynyl]phenyl}dimethylamine 

Relevant academic research and scientific papers

4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors

A series of non-nucleoside adenosine kinase (AK) inhibitors is reported. These inhibitors originated from the modification of 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine (ABT-702). The identification of a linker that would approximate the spatial arrangement found between the pyrimidine ring and the aryl group at C(7) in ABT-702 was a key element in this modification. A search of potential linkers led to the discovery of an acetylene moiety as a suitable scaffold. It was hypothesized that the aryl acetylenes, ABT-702, and adenosine bound to the active site of AK (closed form) in a similar manner with respect to the orientation of the heterocyclic base. Although potent acetylene analogs were discovered based on this assumption, an X-ray crystal structure of 5-(4-dimethylaminophenyl)-6-(6-morpholin-4-ylpyridin-3-ylethynyl)pyrimidin-4-ylamine (16a) revealed a binding orientation contrary to adenosine. In addition, this compound bound tightly to a unique open conformation of AK. The structure-activity relationships and unique ligand orientation and protein conformation are discussed.

Sulfonamides and uses

Sulfonamides of formula I, in which the symbols R1 -R6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.