2021-01- Synthesis and Physico-Chemical Properties of 2-SF5-(Aza)Indoles, A New Family of SF5-Heterocycles
Structural diversity in heterocyclic chemistry is key to unlock new properties and modes of action. In this regard, heterocycles embedding emerging fluorinated substituents hold great promises. Herein is described a strategy to access 2-SF5-(aza)indoles for the first time. The sequence relies on the radical addition of SF5Cl to the alkynyl π-system of 2-ethynyl anilines followed by a cyclization reaction. A telescoped sequence is proposed making this strategy veryappealing and reproducible on gram scale. Downstream functionalizations are also demonstrated, allowing an easy diversification of N- and C3-positions. Ames test, pKa, logP and DSC measurements of several fluorinated 2-Rf-indoles are also disclosed. These studies highlight the strategic advantages that a C2- pentafluorosulfanylated motif impart to a privileged scaffold such as indole.
2021-02- Molecular Mechanisms Underpinning the Circulation and Cellular Uptake of Mycobacterium ulcerans Toxin Mycolactone
Tello Rubio, B.; Bugault, F.; Baudon, B.; Raynal, B.; Brûlé, S.; Morel, J.-D.; Saint-Auret, S.; Blanchard, N.; Demangel, C.; Guenin-Macé, L. Front. Pharmacol. 2021, 12, 733496.
Mycolactone is a diffusible lipid toxin produced by Mycobacterium ulcerans, the causative agent of Buruli ulcer disease. Altough bacterially derived mycolactone has been shown to traffic from cutaneous foci of infection to the bloodstream, the mechanisms underpinning its access to systemic circulation and import by host cells remain largely unknown. We demonstrate that mycolactone specific association to serum albumin and lipoproteins is necessary for its solubilization and is a major mechanism to regulate its bioavailability. Overall, we suggest a new mechanism of transport and cell entry, challenging the dogma that the toxin enters host cells via passive diffusion.
2021-03- Oxetanes and Oxetenes: Fused-Ring Derivatives
Blanchard, N.; Bizet, V.; Brach, N.; Rummler, L.; Kaliappan, K. P. in Comprehensive Heterocyclic Chemistry IV, Vol. 2 (Eds.: D. S. Black, J. Cossy, C. V. Stevens), Elsevier, Oxford, 2022, pp. 257-286.
Fused and spirooxetanes, oxetenes and β-lactones are important classes of compounds that have found numerous applications in various areas of chemistry including medicinal chemistry and total synthesis of natural products. In this chapter, the main achievements from the theoretical and synthetic point of views since its last edition are discussed.
Nous recherchons un post-doc pour de la synthèse de produits naturels par catalyse à l'ADN dans le cadre de l'ANR Smash. Retweetez si vous pouvez. We are seeking for a postdoc associate.
Group website is now updated!
*2 offers for post-doctoral positions
*1 search for candidates for the doctoral school competition in chemical science
We look forward to hearing from you!
More details here: https://bsm.unistra.fr/join-the-group/
@LIMA_UMR7042 @CNRS_Alsace @BizetVincent
The group is looking for candidates for the @unistra 2023 Chemistry Doctoral School Competition ! We propose to further dive into Diels-Alder chemistry. Interested ? Want to know more? Short abstract in the link below. @LIMA_UMR7042
Group website is now updated!
*2 offers for post-doctoral positions
*1 search for candidates for the doctoral school competition in chemical science
We look forward to hearing from you!
More details here: https://bsm.unistra.fr/join-the-group/
@LIMA_UMR7042 @CNRS_Alsace @BizetVincent
A second post-doc position is now available in the group, on total synthesis of natural products analogs. Want to dive into mycolactone chemistry? We're waiting for you!
Details and application on the CNRS website (deadline April 10) https://emploi.cnrs.fr/Offres/CDD/UMR7042-NICBLA-001/Default.aspx?lang=EN @LIMA_UMR7042
You want to join the LIMA @ECPM_Unistra to obtain your PhD? 10 subjects are open in our department to pass the competition of the doctoral school (ED222) @unistra. There is something for everyone (as long as you love molecular chemistry :-)))
http://ed.chimie.unistra.fr/fileadmin/upload/DUN/edsc/03_Financement/2023-Contrats_doctoraux/Final-_2023_Contrats_Doctoraux_-_liste_des_sujets.pdf
Des 3-benzylménadiones (E. Davioud-Charvet, @LIMA) antipaludiques sont testées au @CERMEL (Akim Adegnika, et Steffen Borrmann, Tübingen-Lambaréné) par Stéphanie Blandin (IBMC, @CNRS) et al. sur des souches de Plasmodium spp.
Today we have the pleasure to listen Frédéric Leroux @Leroux_group to tell us more about the development of strategies towards fluoroalkylated building blocks for industrial application
@SynBioF_COBRA @insarouen @univrouen @CNRS_PN
Group website is now updated!
*2 offers for post-doctoral positions
*1 search for candidates for the doctoral school competition in chemical science
We look forward to hearing from you!
More details here: https://bsm.unistra.fr/join-the-group/
@LIMA_UMR7042 @CNRS_Alsace @BizetVincent