Category: 133047-46-8

133047-46-8, Name is 2-Isopropylthiazole-4-carbaldehyde, molecular formula is C7H9NOS, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 133047-46-8, Quality Control of: 2-Isopropylthiazole-4-carbaldehyde

The structure-activity studies leading to the potent and clinically 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 analogues with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chemical 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 muM) and high and sustained plasma concentrations after oral administration in four species. Details of the discovery and preclinical development of ritonavir are described.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Quality Control of: 2-Isopropylthiazole-4-carbaldehyde. In my other articles, you can also check out more blogs about 133047-46-8

Reference£º
Thiazole | C3H3535NS – PubChem,
Thiazole | chemical compound | Britannica

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 133047-46-8, Name is 2-Isopropylthiazole-4-carbaldehyde, molecular formula is C7H9NOS. In a Article，once mentioned of 133047-46-8, category: thiazole

2-pyridyl P1′-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects

A series of symmetry-based HIV protease inhibitors was designed and synthesized. Modification of the core regiochemistry and stereochemistry significantly affected the potency, metabolic stability, and oral bioavailability of the inhibitors, as did the variation of a pendent arylmethyl P3 group. Optimization led to the selection of two compounds, 10c (A-790742) and 9d (A-792611), for advancement to preclinical studies. Both compounds displayed low nanomolar potency against wild type HIV in the presence of human serum, low rates of metabolism in human liver microsomes, and high oral bioavailability in animal models. The compounds were examined in a preclinical model for the hyperbilirubinemia observed with some HIV PIs, and both exhibited less bilirubin elevation than comparator compounds. X-ray crystallographic analyses of the new cores were used to examine differences in their binding modes. The antiviral activity of the compounds against protease inhibitor resistant strains of HIV was also determined.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.category: thiazole. In my other articles, you can also check out more blogs about 133047-46-8

Reference：
Thiazole | C3H3542NS – PubChem,
Thiazole | chemical compound | Britannica