Egbertson, Melissa S. published the artcileNon-Peptide GPIIb/IIIa Inhibitors. 20. Centrally Constrained Thienothiophene α-Sulfonamides Are Potent, Long Acting in Vivo Inhibitors of Platelet Aggregation, Recommanded Product: Pyridine-3-sulfonic acid, the publication is Journal of Medicinal Chemistry (1999), 42(13), 2409-2421, database is CAplus and MEDLINE.
The synthesis and pharmacol. of a potent thienothiophene non-peptide fibrinogen receptor antagonist (I) are reported. Compound I inhibited the aggregation of human gel-filtered platelets with an IC50 of 8 nM and demonstrated an 8-fold improvement in affinity for isolated GPIIb/IIIa receptors over analogs possessing an isoindolinone backbone. Flow cytometry studies revealed that the binding of I to resting platelets is a diffusion-controlled process (kon = 3.3 × 106 M-1 s-1) and that I binds to dog and human platelets with comparable affinity (Kd = 0.04 and 0.07 nM, resp.). Ex vivo platelet aggregation in dogs was completely inhibited by an i.v. dose of 5 mg/kg, and an oral dose of 50-90 mg/kg followed by low daily doses of 10 mg/kg was sufficient to maintain ∼80% inhibition of ex vivo platelet aggregation over several days. Inhibition of ADP-induced platelet aggregation in anesthetized dogs at 77 ± 7% resulted in a moderate 2.5-fold increase in bleeding time, while complete inhibition (100%) resulted in an approx. 10-min bleeding time. Addnl. doses were required to increase the bleeding time to the maximum time allowed in the protocol (15 min), thus indicating a potentially useful and safe separation of efficacy and bleeding time.
Journal of Medicinal Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Recommanded Product: Pyridine-3-sulfonic acid.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem