Kempf, Dale J. published the artcileDiscovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy, HPLC of Formula: 14294-10-1, the publication is Journal of Medicinal Chemistry (1998), 41(4), 602-617, database is CAplus and MEDLINE.
The structure-activity studies leading to the potent and clin. efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable inhibitor A-80987, systematic investigation of peripheral (P3 and P2′) heterocyclic groups designed to decrease the rate of hepatic metabolism provided analogs with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chem. stability toward oxidation while maintaining sufficient aqueous solubility for oral absorption. Optimization of hydrophobic interactions with the HIV protease active site produced ritonavir, with excellent in vitro potency (EC50 = 0.02 μM) and high and sustained plasma concentrations after oral administration in 4 species. Details of the discovery and preclin. development of ritonavir are described.
Journal of Medicinal Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, HPLC of Formula: 14294-10-1.
Referemce:
https://en.wikipedia.org/wiki/Amide,
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