I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 122531-09-3, help many people in the next few years.Quality Control of: 5-Bromo-6-chloro-1H-indole
A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Quality Control of: 5-Bromo-6-chloro-1H-indole, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 122531-09-3, Name is 5-Bromo-6-chloro-1H-indole, molecular formula is C8H5BrClN. In a Article, authors is Edmonds, David J.£¬once mentioned of 122531-09-3
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5?-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described. Derivatives of the previously described 5-aryl-indole-3-carboxylic acid clinical candidate (1) were examined with the goal of reducing glucuronidation rate and minimizing renal excretion. Compounds 10 (PF-06679142) and 14 (PF-06685249) exhibited robust activation of AMPK in rat kidneys as well as desirable oral absorption, low plasma clearance, and negligible renal clearance in preclinical species. A correlation of in vivo renal clearance in rats with in vitro uptake by human and rat renal organic anion transporters (human OAT/rat Oat) was identified. Variation of polar functional groups was critical to mitigate active renal clearance mediated by the Oat3 transporter. Modification of either the 6-chloroindole core to a 4,6-difluoroindole or the 5-phenyl substituent to a substituted 5-(3-pyridyl) group provided improved metabolic stability while minimizing propensity for active transport by OAT3.
I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 122531-09-3, help many people in the next few years.Quality Control of: 5-Bromo-6-chloro-1H-indole
Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles