Young, Mary Beth published the artcileDiscovery and Evaluation of Potent P1 Aryl Heterocycle-Based Thrombin Inhibitors, Computed Properties of 724710-02-5, the publication is Journal of Medicinal Chemistry (2004), 47(12), 2995-3008, database is CAplus and MEDLINE.
In an effort to discover potent, clin. useful thrombin inhibitors, a rapid analog synthetic approach was used to explore the P1 region. Various benzylamines were coupled to a pyridine/pyrazinone P2-P3 template. One compound, i.e. 2-[6-chloro-3-(2,2-difluoro-2-pyridin-2-yl-ethylamino)-2-oxo-2H-pyrazin-1-yl]-N-(2-[1,2,3]thiadiazol-4-yl-benzyl)acetamide, was found to have a thrombin Ki of 0.84 nM. A study of ortho-substituted five-membered-ring heterocycles was undertaken and subsequently demonstrated that the o-triazole and tetrazole rings were optimal. Combination of these potent P1 aryl heterocycles with a variety of P2-P3 groups produced a compound with an extraordinary thrombin inhibitory activity of 1.4 pM. It is hoped that this potency enhancement in P1 will allow for more diversification in the P2-P3 region to ultimately address addnl. pharmacol. concerns.
Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C11H10N4, Computed Properties of 724710-02-5.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics