[Nirmatrelvir/ritonavir (Paxlovid®), a treatment for Covid-19]. / Le nirmatrelvir-ritonavir (Paxlovid®), un traitement contre la Covid-19.

The nirmatrelvir-ritonavir (Paxlovid®) is a treatment against Covid-19 available in pharmacies since February 4, 2022. Administered orally, it is intended only for people at very high risk of contracting one or more severe forms of the disease.

Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.

Our previous studies have shown that several 7-substituted-4-imidazolylflavans are potent inhibitors of aromatase. These compounds were designed considering the anti-aromatase effect of some natural flavonoids and the importance of an azole ring for synthetic inhibitors such as letrozole or anastrozole towards binding to the heme iron of aromatase. In this study, we report the optimization of these lead compounds by the modulation of flavan A ring. The resulting 7,8-benzo-4-imidazolylflavans were tested in order to assess their ability to inhibit aromatase. Biological data concerning enantiomers obtained from the chiral separation of the racemate compound 4-imidazolyl-7-methoxyflavan are also presented.

New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.

Some natural compounds such as flavonoids are known to possess a moderate inhibitory activity against aromatase, this enzyme being an interesting target for hormone-dependent breast cancer treatment. It has been demonstrated that the modulation of flavonoid skeleton could increase anti-aromatase effect. Therefore, new 7,8-benzoflavanones were synthesized and tested for their activity toward aromatase inhibition. It was observed that the introduction of a benzo ring at position C-7 and C-8 on flavanone skeleton led to new potent aromatase inhibitors, the resulting 7,8-benzoflavanones being until nine times more potent than aminogluthetimide (the first aromatase inhibitor used clinically).