Design, Synthesis, and Biological Activity of New N-(Phenylmethyl)-benzoxazol-2-thiones as Macrophage Migration Inhibitory Factor (MIF) Antagonists: Efficacies in Experimental Pulmonary Hypertension

Autor: Marc Humbert, Alice Huertas, Gérald Simonneau, Gaël Jalce, Ly Tu, Christophe Guignabert, Elie Fadel, Raphaël Thuillet, Guillaume Bernadat, Carole Phan, Bernardin Akagah, Morane Le Hiress

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2018, 61 (7), pp.2725-2736. ⟨10.1021/acs.jmedchem.7b01312⟩
Journal of Medicinal Chemistry, 2018, 61 (7), pp.2725-2736. ⟨10.1021/acs.jmedchem.7b01312⟩

Macrophage migration inhibitory factor (MIF) is a key pleiotropic mediator and a promising therapeutic target in cancer as well as in several inflammatory and cardiovascular diseases including pulmonary arterial hypertension (PAH). Here, a novel seri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6eb93576e781fbc8e669719b29bb43bf
https://pubmed.ncbi.nlm.nih.gov/29526099

Synthesis of 5,15-diarylporphyrins via orthoesters condensation with aryldipyrromethanes

Autor: Anh Tuan Lormier, Bernardin Akagah, Laurent Ferrié, Zahra Abada, Bruno Figadère

Publikováno v: Tetrahedron Letters. 52:3175-3178

General access to 5,15-diarylporphyrins in two steps is described. Generalization of this approach to tetra-substituted porphyrins allows the reproducible preparation of compounds, in some cases with high yields for porphyrins, which can be used in p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::979976d72aa6806a4623c75a13905cf8
https://doi.org/10.1016/j.tetlet.2011.04.028

Regio- and diastereocontrolled preparative oxidation of methyloctalones by a biomimetic porphyrin catalyst

Autor: François Estour, Bernardin Akagah, Philippe Vérité, Mohammed Nour, Sabine Ménager, Olivier Lafont, Pedro Lameiras, Christian Cavé

Publikováno v: Chirality. 16:398-403

Both enantiomers of methyloctalone were oxidized by a biomimetic manganese/porphyrin/imidazole catalytic system in order to obtain sufficient amounts of various model metabolites. The double bond proved to be less sensitive than the ring methylenes.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c273a3371cd087ed8374fbb42da253d5
https://doi.org/10.1002/chir.20043

Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives

Autor: Anh Tuan Lormier, Sandrine Cojean, Philippe M. Loiseau, Zahra Abada, Bruno Figadère, Bernardin Akagah, Laurent Ferrié, Sébastien Pomel

Publikováno v: European journal of medicinal chemistry. 67

Importance of heme in African trypanosomes, Leishmania sp. and Plasmodium sp. metabolisms justifies considering the potential of porphyrins and their precursors and derivatives as potential antiparasitic agents by interfering with heme metabolism. Co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee0ffe20a1619b137cee514ed1187ae6
https://pubmed.ncbi.nlm.nih.gov/23851117

Synthesis of Models of Metabolites: Oxidation of Variously Substituted Chromenes Including Acronycine, by a Porphyrin Catalytic System

Autor: Elisabeth Seguin, Bernardin Akagah, François Tillequin, François Estour, Philippe Vérité, Olivier Lafont

Publikováno v: Journal of Heterocyclic Chemistry
Journal of Heterocyclic Chemistry, Wiley, 2005, 42 (7), pp.1267-1272. ⟨10.1002/jhet.5570420704⟩

International audience; The influence of chemical neighbouring on oxidation of substituted 2,2‐dimethylchromenes derivatives 5‐8 by a biomimetic catalytic system was first studied. It was then applied to acronycine an anti‐cancer drug in order

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcfacb7cd9f9ece39848d3360b35c7c0
https://doi.org/10.1002/chin.200614138