Tag Archives: AstraZeneca

Improving Solubility using X-ray crystal structure data

A recent publication from AstraZeneca provides a really interesting overview of the approach that they took to optimise the solubility of a series of GPR119 agonists. The initial lead compound 2 was only poorly soluble but, by obtaining small molecule … Continue reading

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Drug discovery approaches to minimise drug induced liver injury in man

The recent literature has seen a flurry of papers describing the issue of, and potential approaches to minimising the incidence of, drug-induced liver injury (DILI) in the clinic.   It is well recognised that attrition throughout the development pipeline is often … Continue reading

Posted in Med Chem Strategy, Toxicology | Tagged , , , , , , , , , , , , , , , , | 3 Comments

Atropisomerism in Drug Discovery

Following up on their earlier mini-review, the authors of this recent paper outline their work at Boehringer Ingelheim on developing methodology and strategies for dealing with the issue of atropisomerism in drug discovery.  The authors highlight the fact that, whilst the … Continue reading

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