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N-glucuronidation: the human element

Metabolite Tales Blog

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. Tukey, Ryoichi Fujiwara. Antimicrob Agents Chemother.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

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. 16 This concludes our exploration of metabolism of last year’s FDA approved small molecule drugs.

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Metabolism of five membered nitrogen containing heterocycles

Metabolite Tales Blog

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.

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Breaking C-F bonds in drugs

Metabolite Tales Blog

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.

Drugs 52