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Effect of ophiopogonin D on the pharmacokinetics and transport of cryptotanshinone during their co?administration and the potential mechanism

Chemical Biology and Drug Design

The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. The Caco-2 cells were employed to evaluate the transport of cryptotanshinone, and the metabolic stability was studied in the rat liver microsomes.

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Targeted modification of furan?2?carboxaldehydes into Michael acceptor analogs yielded long?acting hemoglobin modulators with dual antisickling activities

Chemical Biology and Drug Design

However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

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]. Balazs et al.,

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

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]. Balazs et al.,

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Pharmacokinetic study of the interaction between luteolin and magnoflorine in rats

Chemical Biology and Drug Design

Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. CaCO-2 cell transwell assay was employed for transport evaluation, and the metabolic stability of luteolin and CYP3A activity were assessed in rat liver microsomes.

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How the AI revolution can accelerate early drug discovery

Drug Target Review

Complex challenges such as metabolic stability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. He has published 22 scientific articles and has a h-index of 13. Matthew is a chartered chemist.

Drugs 105
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Efficient trajectories

Molecular Design

I'll examine an article entitled ‘Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations’ (YL2018) in this post and I should note that the article title reminded me that abseiling has been described as the second fastest way down the mountain.