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Rational Drug Design and Synthesis of New α-Santonin Derivatives as Potential COX-2 Inhibitors

Rational Drug Design and Synthesis of New α-Santonin Derivatives as Potential COX-2 Inhibitors

Adriana Coricello, Asma El-Magboub, Marian Luna, Angela Ferrario, Ian S Haworth, Charles J Gomer, Francesca Aiello, James D Adams

Bioorg Med Chem Lett. 2018 Apr 1;28(6):993-996.

PMID: 29501395

Abstract:

Sesquiterpene compounds are widely known for their numerous pharmacological activities. Herein the focus of the authors was on α-Santonin, a sesquiterpene lactone from the Artemisia genus: the aim was to determine whether α-Santonin could be considered in the treatment of inflammation and pain. To this purpose, a small series of derivatives was designed and screened in silico against the enzyme COX-2 along with the parent compound. Drug-likeness parameters were also assessed. The compounds were eventually synthesized, and few were tested to determine their efficacy in the inhibition of COX-2 activity and expression. Overall, compound A2 was the only one with a detectable inhibitory potential of COX-2 activity whilst two of its ether derivatives demonstrated improved ability in the inhibition of COX-2 expression.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP481061	α-Santonin		481-06-1	Price

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