(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators

Autor: Marouan Rami, Jean-Yves Winum, Claudiu T. Supuran, Patricia Melnyk, Saïd Yous

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 224-229 (2019)

Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I,

Externí odkaz: https://doaj.org/article/e55317ea4e174352b997ce004b41d544

Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT

Autor: Romain, Duroux, Marouan, Rami, Elodie, Landagaray, Mohamed, Ettaoussi, Daniel-Henri, Caignard, Philippe, Delagrange, Patricia, Melnyk, Saïd, Yous

Publikováno v: European journal of medicinal chemistry. 141

We recently reported a series of naphthofuranic compounds as constrained agomelatine analogues. Herein, in order to explore alternative ethyl amide side chain rigidification, naphthocyclopentane and quinolinocyclopentane derivatives with various acet

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b8d98df03832e329a93a83a1346c0b3f
https://pubmed.ncbi.nlm.nih.gov/29102176

Hypoxia-Targeting Carbonic Anhydrase IX Inhibitors by a New Series of Nitroimidazole-Sulfonamides/Sulfamides/Sulfamates

Autor: Marouan Rami, Jean-Yves Winum, Philippe Lambin, Simona Maria Monti, Ludwig Dubois, Giuseppina De Simone, Nanda-Kumar Parvathaneni, Vincenzo Alterio, Claudiu T. Supuran, Simon J. A. van Kuijk

Publikováno v: Journal of Medicinal Chemistry, 56(21), 8512-8520. American Chemical Society
Journal of Medicinal Chemistry; Vol 56
Journal of medicinal chemistry (Online) 56 (2013): 8512–8520. doi:10.1021/jm4009532
info:cnr-pdr/source/autori:Rami M.; Dubois L.; Parvathaneni N.-K.; Alterio V.; Van Kuijk S.J.A.; Monti S.M.; Lambin P.; De Simone G.; Supuran C.T.; Winum J.-Y./titolo:Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides%2Fsulfamides%2Fsulfamates/doi:10.1021%2Fjm4009532/rivista:Journal of medicinal chemistry (Online)/anno:2013/pagina_da:8512/pagina_a:8520/intervallo_pagine:8512–8520/volume:56
Journal of Medicinal Chemistry

A series of nitroimidazoles incorporating sulfonamide/sulfamide/sulfamate moieties were designed and synthesized as radio/chemosensitizing agent targeting the tumor-associated carbonic anhydrase (CA) isoforms IX and XII. Most of the new compounds wer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c19bb34ec93a27cb43769d10984bdc09
https://doi.org/10.1021/jm4009532

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I)

Autor: Mohamed Ettaoussi, Philippe Delagrange, Jean A. Boutin, Pierre Renard, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Marouan Rami, Saïd Yous, Daniel-Henri Caignard

Publikováno v: European Journal of Medicinal Chemistry. 49:310-323

As part of our ongoing interest in developing new melatoninergic ligands bearing the same pharmacological profile as agomelatine, we focused our attention on this compound as a lead. Several chemical modifications have been performed on positions C-3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87e7ea27e686b75cb0b968101d32906e
https://doi.org/10.1016/j.ejmech.2012.01.027

Sulfonamides incorporating boroxazolidone moieties are potent inhibitors of the transmembrane tumor-associated carbonic anhydrase isoforms IX and XII

Autor: Alfonso Maresca, Andrea Scozzafava, Claudiu T. Supuran, Fatma-Zhora Smaine, Jean-Louis Montero, Marouan Rami, Jean-Yves Winum

Publikováno v: Bioorganic & Medicinal Chemistry Letters; Vol 21
Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2011, 21, pp.2975-2979. ⟨10.1016/j.bmcl.2011.03.055⟩

A new series of sulfonamides was synthesized by the reaction of the boroxazolidone complex of l-lysine with isothiocyanates incorporating sulfamoyl moieties and diverse organic scaffolds. The obtained thioureas have been investigated as inhibitors of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::71a422001fc050991d369723a159df00