Duroux, Romain published the artcileAntagonists of the adenosine A2A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity, Application In Synthesis of 197958-29-5, the publication is European Journal of Medicinal Chemistry (2018), 151-163, database is CAplus and MEDLINE.
The authors have recently reported a series of 2-furoyl-benzoxazoles as potential A2A adenosine receptor (A2AR) antagonists. Two hits were identified with interesting pharmacokinetic properties but were find to bind the hA2AR receptor in the micromolar-range. Herein, to enhance affinity toward the hA2AR, the authors explored the C5- and C7-position of the hits based on docking studies. These modifications led to compounds with nanomolar-range affinity (e.g., 6a (2,7-di(furan-2-yl)benzoxazol-5-amine), Ki = 40 nM) and high antagonist activity (e.g., 6a, IC50 = 70.6 nM). Selected compounds also exhibited interesting in vitro DMPK (Drug Metabolism and Pharmacokinetics) properties including high solubility and low cytotoxicity. Therefore, the benzoxazole ring appears as a highly effective scaffold for the design of new A2A antagonists.
European Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application In Synthesis of 197958-29-5.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem