New azole antifungals with a fused triazinone scaffold

Autor: David Montoir, Isabelle Ourliac-Garnier, Aurélien Planchat, Kossi Efouako Soklou, Carine Picot, Rémi Guillon, Sophie Gazzola, Alain Tonnerre, Cédric Logé, Fabrice Pagniez, Patrice Le Pape

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2020, 189, pp.112082. ⟨10.1016/j.ejmech.2020.112082⟩

International audience; We identified a new series of azole antifungal agents bearing a pyrrolotriazinone scaffold. These compounds exhibited a broad in vitro antifungal activity against pathogenic Candida spp. (fluconazole-susceptible and fluconazol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c43babd6c0314939c9e45a6a3fd0ca5c
https://hal.archives-ouvertes.fr/hal-03412473

Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90

Autor: Alain Tonnerre, Marc-Antoine Bazin, Sophie Barillé-Nion, Muriel Duflos, Philippe Juin, David Montoir

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 2016, 119, pp.17-33. ⟨10.1016/j.ejmech.2016.04.050⟩
European Journal of Medicinal Chemistry, Elsevier, 2016, 119, pp.17-33. ⟨10.1016/j.ejmech.2016.04.050⟩

International audience; Hsp90 is an ATP-dependent chaperone known to be overexpressed in many cancers. This way, Hsp90 is an important target for drug discovery. Novobiocin, an aminocoumarin antibiotic, was reported to inhibit Hsp90 targeting C-termi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0a281a0a905ddeb26b1b375b11c0e47
https://doi.org/10.1016/j.ejmech.2016.04.050

Differential Functionalization of 1,6-Naphthyridin-2(1H)-ones through Sequential One-Pot Suzuki-Miyaura Cross-Couplings

Autor: Alain Tonnerre, Muriel Duflos, Marc-Antoine Bazin, David Montoir

Publikováno v: European Journal of Organic Chemistry. 2014:1487-1495

A practical synthesis of 7-chloro-3-iodo-1-methyl-1,6-naphthyridin-2(1H)-one is described that starts from 2-chloro-4-(methylamino)nicotinaldehyde. The dihalo compound then undergoes sequential, site-selective Suzuki–Miyaura cross-coupling reaction

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6a13b0afeb3e6a678aa29aa32f9c774e
https://doi.org/10.1002/ejoc.201301631

ChemInform Abstract: Differential Functionalization of 1,6-Naphthyridin-2(1H)-ones Through Sequential One-Pot Suzuki-Miyaura Cross-Couplings

Autor: Marc-Antoine Bazin, Muriel Duflos, Alain Tonnerre, David Montoir

Publikováno v: ChemInform. 45

A practical synthesis of 7-chloro-3-iodo-1-methyl-1,6-naphthyridin-2(1H)-one is described that starts from 2-chloro-4-(methylamino)nicotinaldehyde. The dihalo compound then undergoes sequential, site-selective Suzuki–Miyaura cross-coupling reaction

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3bcfbd64d385edb826f93abd908e5baf
https://doi.org/10.1002/chin.201449157

Discovery of a Novel Broad-Spectrum Antifungal Agent Derived from Albaconazole

Autor: Fabrice Pagniez, Alain Tonnerre, Patrice Le Pape, Thierry Besson, Carine Picot, Damien Hédou, Cédric Logé, Muriel Duflos, Rémi Guillon, Elizabeth Chosson

Publikováno v: ACS Medicinal Chemistry Letters
ACS Medicinal Chemistry Letters, American Chemical Society, 2013, 4 (2), pp.288-292. ⟨10.1021/ml300429p⟩

Synthesis of a strict structural analogue of albaconazole in which the quinazolinone ring is fused by a thiazole moiety led to the discovery of a new triazole with broad-spectrum antifungal activity. Compound I exhibited high in vitro activity agains

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63964d196e6b1ac81fd1d3b921fb6fe0
https://hal.archives-ouvertes.fr/hal-01015468