Metabolite Tales Blog
AUGUST 2, 2023
To curb O -glucuronidation at that position, a gem-dimethyl group was incorporated, which not only boosted metabolic stability but also resulted in increased potency of “compound 17” An earlier example of how to manage glucuronidation by steric hindrance is illustrated in “compound 25” in the paper by Zhang et al.,
Metabolite Tales Blog
DECEMBER 13, 2023
N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Glucuronidation is the most common phase II reaction observed in the metabolism of drugs in humans. Derun Li, David L. McGowan, Catherine White et al.
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Metabolite Tales Blog
APRIL 4, 2023
Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Metabolism of orally administered tauroursodeoxycholic acid in patients with primary biliary cirrhosis.
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13].
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13].
Metabolite Tales Blog
MARCH 1, 2023
This mix of properties makes azoles very versatile in medicinal chemistry and each tend to have quirks of metabolism that we highlight in this blog. that highlighted specific biotransformations of five-membered heteroaromatic rings, 1 we have sought to highlight additional examples and recent understanding in their metabolism.
Metabolite Tales Blog
MAY 12, 2023
This was surprising given that replacement of a phenyl with a pyrimidine and fluorination of aryl or heteroaryl rings are techniques often used to increase metabolic stability. Chemical Reviews 2021 121 (8), 4678-4742, [link] Take a look at our other blogs The post Breaking C-F bonds in drugs appeared first on Hypha Discovery.
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