Procopiou, Panayiotis A. published the artcileSynthesis and Structure-Activity Relationships of Indazole Arylsulfonamides as Allosteric CC-Chemokine Receptor 4 (CCR4) Antagonists, Computed Properties of 221202-34-2, the main research area is indazole arylsulfonamide allosteric CC chemokine receptor 4 antagonist preparation; structure activity relationship solubility clearance human CCR4 antagonist; crystal mol structure indazole thiophenesulfonamide.
A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy- or hydroxyl- containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analogs being preferred. The most potent N3-substituent was 5-chlorothiophene-2-sulfonamide. N1 meta-substituted benzyl groups possessing an α-amino-3-[(methylamino)acyl]- group were the most potent N1-substituents. Strongly basic amino groups had low oral absorption in vivo. Less basic analogs, such as morpholines, had good oral absorption; however, they also had high clearance. The most potent compound with high absorption in two species was analog I (GSK2239633A), which was selected for further development. Aryl sulfonamide antagonists bind to CCR4 at an intracellular allosteric site denoted site II. X-ray diffraction studies on two indazole sulfonamide fragments suggested the presence of an important intramol. interaction in the active conformation.
Journal of Medicinal Chemistry published new progress about Acidity. 221202-34-2 belongs to class nitriles-buliding-blocks, name is 2,3-Difluoro-6-methoxybenzonitrile, and the molecular formula is C8H5F2NO, Computed Properties of 221202-34-2.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts