Matulenko, Mark A. published the artcile4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors, Synthetic Route of 17259-32-4, the main research area is aminoarylarylethynylpyrimidine derivative preparation structure adenosine kinase inhibitor analgesic pain.
A series of nonnucleoside 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 approx. 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 (I) 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.
Bioorganic & Medicinal Chemistry published new progress about Analgesics. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Synthetic Route of 17259-32-4.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem