Leahy, James W. published the artcileDiscovery of a Novel Series of Potent and Orally Bioavailable Phosphoinositide 3-Kinase γ Inhibitors, HPLC of Formula: 1033743-83-7, the publication is Journal of Medicinal Chemistry (2012), 55(11), 5467-5482, database is CAplus and MEDLINE.
The phosphoinositide 3-kinases (PI3Ks) have been linked to an extraordinarily diversified group of cellular functions making these enzymes compelling targets for the treatment of disease. A large body of evidence has linked PI3Kγ to the modulation of autoimmune and inflammatory processes making it an intriguing target for drug discovery. A high-throughput screening (HTS) campaign revealed two hits that were nominated for further optimization studies. The in vitro activity of the first HTS hit, I, designated as the sulfonylpiperazine scaffold, was optimized utilizing structure-based design. However, nonoptimal pharmacokinetic properties precluded this series from further studies. An overlay of the x-ray structures of the sulfonylpiperazine scaffold and the second HTS hit, II, within their complexes with PI3Kγ revealed a high degree of overlap. This feature was utilized to design a series of hybrid analogs including advanced leads such as III with desirable potency, selectivity, and oral bioavailability.
Journal of Medicinal Chemistry published new progress about 1033743-83-7. 1033743-83-7 belongs to piperazines, auxiliary class Piperazine,Boronic acid and ester,Sulfamide,Benzene,Amide,Boronate Esters,Boronic Acids,Boronic acid and ester, name is tert-Butyl 4-((3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)sulfonyl)piperazine-1-carboxylate, and the molecular formula is C21H33BN2O6S, HPLC of Formula: 1033743-83-7.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics