Inactivation of Malaria Parasites in Blood: PDT vs Inhibition of Hemozoin Formation

Malaria causes hundreds of thousands of human deaths every year, and the World Health Assembly has made it a priority. To help eliminate this disease, there is a pressing need for the development and implementation of new strategies to improve the prevention and treatment, due in part to antimalarial drug resistances. This chapter focuses on two strategies to inactivate the malaria parasite in blood, which are photodynamic therapy (PDT) and inhibition of hemozoin formation. The PDT strategy permits either a control of the proliferation of mosquito larvae to develop some photolarvicides for the prevention or a photoinactivation of the malaria parasite in red blood cells (RBCs) to minimize infection transmission by transfusion. The inhibition of hemozoin formation strategy is used for the development of new antimalarial drug by understanding its formation mechanism

Low-cost and multi-gram scale synthesis of chiral Nβ-Boc protected α-Nα-hydrazino diesters

International audienceAn efficient and general low-cost method is described to obtain chiral Nβ-Boc protected α-Nα-hydrazino diester building-blocks (orthogonally and non-orthogonally protected diesters) on multi-gram scale (30 mmol) using two successive SN2 reactions. This method is also convenient for the introduction of both polar and nonpolar side chains on the Nα-atom and represents an inexpensive and attractive alternative compared to the more expensive method using commercial oxaziridine reagents for N-amination of α-amino acid

Synthèses énantiosélectives à partir de chirons à 5 chaînons (carbosucres et produits naturels de la famille des cuparanes et des herbertanes)

Ce travail développe différentes stratégies et tactiques pour la synthèse énantiosélective de carbosucres et de produits naturels à partir de briques moléculaires énantiopures obtenues par dédoublement enzymatique de cétones cycliques à 5 chaînons. Il est présenté en 3 chapitres.Le premier chapitre est consacré à la synthèse énantiosélective de carbosucres inédits. Le second chapitre aborde les synthèses énantiosélectives du (-)-acétate de tochuinyle, du (-)-acétate de dihydrotochuinyle et de la (+)- -cuparènone, trois sesquiterpènes naturels de la famille des Cuparanes possédant deux centres quaternaires contigus sur le cycle à 5 chaînons. Le troisième chapitre est consacré à la synthèse énantiosélective du (-)- -herbertènol, (-)-herbertènediol et du (+)-1,14-dihydroxyherbertène, sesquiterpènes naturels de la famille des Herbertanes.AIX-MARSEILLE3-BU Sc.St Jérô (130552102) / SudocSudocFranceF

Distorted five-coordinate square pyramidal geometry of a cadmium(II) complex containing a 2-methylimidazole ligand: Crystal structure and axial ligand effect on spectroscopic properties

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Use of lipase-catalyzed kinetic resolution for the enantioselective approach toward sesquiterpenes containing quaternary centers: the cuparane family

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Multigram‐scale HPLC enantioseparation as a rescue pathway for circumventing racemization problem during enantioselective synthesis of ethyl 3,4‐dihydro‐ 2H ‐1,4‐benzoxazine‐2‐carboxylate

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Enantiopure ethyl 2,3‐dibromopropionate: Enantioselective synthesis vs preparative HPLC enantioseparation of racemate on multigram scale

International audienceRacemic ethyl 2,3‐dibromopropionate, commercially available at low price, is a key intermediate used in the synthesis of several heterocycle fragments, which are present in many biologically active compounds. Surprisingly, the enantiomers are not commercially available and have never been described in the literature. In this work, we undertook two different strategies to obtain these enantiomers, which are enantioselective synthesis and preparative HPLC enantioseparation of commercially available racemate on multigram scale. The first strategy has proved inadequate because racemization occurred during the synthesis (ee ≈ 9‐50%). Conversely, the second strategy produced a very good enantioseparation of commercially available racemate (ee > 99.5% for both enantiomers) on multigram scale

Synthesis and Conformational Analysis of 1:1 [α/α- N α -Bn-Hydrazino] and 1:1 [α- N α -Bn-Hydrazino/α] Trimers: Determination of the Δ δ Value for the γ-Turn Structuration

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Total synthesis of high loading capacity PEG-based supports: evaluation and improvement of the process by use of ultrafiltration and PEG as a solvent

International audienceThe present work deals with the total synthesis of high loading capacity PEG supports with attention focused on improving the greenness of all the steps. The systematic calculation of green metrics offers an opportunity to evaluate the greenness and then to improve the process. To evidence such an improvement, the evaluation of the optimized processes was compared with that of the classical ones