Peptide-Alkoxyamine Drugs: An Innovative Approach to Fight Schistosomiasis: "Digging Their Graves with Their Forks".

The expansion of drug resistant parasites sheds a serious concern on several neglected parasitic diseases. Our recent results on cancer led us to envision the use of peptide-alkoxyamines as a highly selective and efficient new drug against schistosome adult worms, the etiological agents of schistosomiasis. Indeed, the peptide tag of the hybrid compounds can be hydrolyzed by worm's digestive enzymes to afford a highly labile alkoxyamine which homolyzes spontaneously and instantaneously into radicals-which are then used as a drug against Schistosome adult parasites.

Hybrid Peptide-Alkoxyamine Drugs: A Strategy for the Development of a New Family of Antiplasmodial Drugs.

The emergence and spread of drug-resistant parasites shed a serious concern on the worldwide control of malaria, the most important tropical disease in terms of mortality and morbidity. This situation has led us to consider the use of peptide-alkoxyamine derivatives as new antiplasmodial prodrugs that could potentially be efficient in the fight against resistant malaria parasites. Indeed, the peptide tag of the prodrug has been designed to be hydrolysed by parasite digestive proteases to afford highly labile alkoxyamines drugs, which spontaneously and instantaneously homolyse into two free radicals, one of which is expected to be active against .

Design of a Targeting and Oxygen-Independent Platform to Improve Photodynamic Therapy: A Proof of Concept.

Photodynamic therapy (PDT) is a promising technique to treat different kinds of disease especially cancer. PDT requires three elements: molecular oxygen, a photoactivatable molecule called the photosensitizer (PS), and appropriate light. Under illumination, the PSs generate, in the presence of oxygen, the formation of reactive oxygen species including singlet oxygen, toxic, which then destroys the surrounding tissues.

Atypical Reaction Media and Organized Systems for the Synthesis of Low-Substitution Sugar Esters.

Sugar esters are non-ionic surfactants with amphiphilic properties of interest for the formulation of various products in the fields of detergents, foods, medicines, pharmaceuticals, agriculture, and cosmetics. The properties of sugar esters depend on their degree of substitution (we consider degrees of substitution between 1 and 3 here) which guides their use. Sugar esters are biodegradable and non-toxic, and the demand for these compounds is high and continuing to increase.

Detection of Bisphenol A in aqueous medium by screen printed carbon electrodes incorporating electrochemical molecularly imprinted polymers.

Electrochemical molecularly imprinted polymers (e-MIPs) were for the first time introduced in screen-printed carbon electrodes (SPCE) as the sensing element for the detection of an organic pollutant. To play this sensing role, a redox tracer was incorporated inside the binding cavities of a cross-linked MIP, as a functional monomer during the synthesis step. Ferrocenylmethyl methacrylate was used for this purpose.

How intramolecular hydrogen bonding (IHB) controls the C-ON bond homolysis in alkoxyamines.

Recent amazing results (Nkolo et al., Org. Biomol.

C-ON bond homolysis of alkoxyamines: when too high polarity is detrimental.

Throughout the last decade, the effect of electron withdrawing groups (EWGs) has been known to play a role - minor or moderate depending on the nitroxyl fragment RRNO - in the change in the homolysis rate constant (k) for C-ON bond homolysis in alkoxyamines (RRNOR). It has been shown that the effect of EWGs on k is described by a linear relationship with the electrical Hammett constant σ. Since then, linear multi-parameter relationships f(σ,ν,σ) have been developed to account for the effects involved in the changes in k, which are the stabilization of the released radical (σ) and the bulkiness (ν) and polarity (σ) of the alkyl fragment.

Normal, Leveled, and Enhanced Steric Effects in Alkoxyamines Carrying a β-Phosphorylated Nitroxyl Fragment.

The design of new RRNOR alkoxyamines for various applications relies on the accurate prediction of two kinetic parameters, the C-ON bond homolysis rate constant (k) and its re-formation rate constant (k). Relationships to describe the steric and polar effects of the RRNO fragment ruling k have been developed. For all cyclic nitroxyl fragments, the steric effect is described as the sum of the bulkiness of the R and R groups (i.

A New Benzophenanthridine Alkaloid from Caloncoba glauca.

Three alkaloids including a new one, N-formyldihydrochelerythrine (1), together with four other known compounds were isolated from the stem bark of Caloncoba glauca. The structure of the new compound was elucidated from spectroscopic and mass spectrometric evidence. This is the first report of alkaloids from the genus Caloncoba.

The β-phosphorus hyperfine coupling constant in nitroxides: 6. Solvent effects in non-cyclic nitroxides.

In two recent articles (Org. Biomol. Chem.

Essential oil of Plectranthus tenuicaulis leaves from Gabon, source of (R),(E)-6,7-epoxyocimene. An unusual chemical composition within the genus Plectranthus.

Water distilled essential oils from leaves of Plectranthus tenuicaulis (Hook. f.) J.

Chemical composition and biological activities of Santiria trimera (Burseraceae) essential oils from Gabon.

Water-distilled essential oils from leaves and bark of Santiria trimera (Oliv.) Aubrév. (Burseraceae) collected in Gabon were analyzed using capillary GC-FID and GC-MS.

Chemical composition and antimicrobial activity of the essential oils of leaves, roots and bark of Glossocalyx staudtii.

The chemical composition of the essential oils obtained by hydrodistillation from air dried leaves, bark and roots of Glossocalyx staudtii Engl. grown in Gabon was analyzed by GC and GC-MS. The essential oil content was 0.