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.,
Drug Target Review
JUNE 12, 2023
Chemistry42 is a customisable and fully automated software platform launched in 2020 that integrates generative AI algorithms with computational and medicinal chemistry methods to generate novel molecules with drug-like properties, sometimes in a matter of days. How was ISM6331 generated and optimised using Chemistry42?
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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]. Nagasaka et al.,
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]. Nagasaka et al.,
Metabolite Tales Blog
APRIL 4, 2023
Deuteration at this position was found to block generation of a less selective primary amide metabolite in vivo and increase metabolic stability. The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans. Journal of Medicinal Chemistry 63 (13), 6679-6693.
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. References [1] Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. Benjamin M. Johnson, Yue-Zhong Shu, Xiaoliang Zhuo, and Nicholas A.
Metabolite Tales Blog
MARCH 1, 2023
2020, 25, 4309 [link] 20 Drug Metab. 44, 797–814 [link] Take a look at our other blogs The post Metabolism of five membered nitrogen containing heterocycles appeared first on Hypha Discovery. 1994, 22, 651-658 [link] 17b Drug Metab. 1994, 22, 659-662 [link] 18a Xenobiotica , 1986, 16, 11-20 [link] 18b Wood and Fibre Science.
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