Výsledky vyhledávání

Synthesis and Biological Evaluation of C-5 Methyl Substituted 4-Arylthio and 4-Aryloxy-3-Iodopyridin-2(1H)-one Type Anti-HIV Agents

Autor: Marie-Pierre de Béthune, Said Oumouch, Patrice Palandjian, Jerome Emile Georges Guillemont, Daniel Vernier, Kurt Hertogs, Koen Andries, Chi Hung Nguyen, Laurence Queguiner, David S. Grierson, Abdellah Benjahad, Laurence F B Decrane

Publikováno v: Journal of medicinal chemistry

A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin-2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb4b3260eeaf39908174f455f48fc404
https://doi.org/10.1021/jm900802y

Zobrazit plný text záznamu

4-Benzyl- and 4-Benzoyl-3-dimethylaminopyridin-2(1H)-ones, a New Family of Potent Anti-HIV Agents: Optimization and in Vitro Evaluation against Clinically Important HIV Mutant Strains

Autor: Karine Courte, Marie-Pierre De Bethune, Rudi Pauwels, Jérome Guillemont, Csoka Imre Christian Francis, Chi Hung Nguyen, Alain Poncelet, Emile Bisagni, Sophie Coupa, David S. Grierson, Dominique Mabire, Abdellah Benjahad, Koen Andries, Claude Monneret

Publikováno v: Journal of medicinal chemistry

The 4-benzyl and 4-benzoyl-3-dimethylaminopyridinones 13 and 14 are representatives of a new class of highly potent non nucleoside type inhibitors of HIV-1 reverse transcriptase. To conduct SAR studies on these two lead compounds, 102 new analogues w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26af9a522cccb06a81c98206ba082c3b
https://doi.org/10.1021/jm0407658

Zobrazit plný text záznamu

SYNTHESIS OF 3-ALKYL PIPERAZIN-2-ONE NUCLEOSIDES WITH POTENTIAL ANTIRETROVIRAL ACTIVITY

Autor: Pierre Krausz, Abdellah Benjahad, Claudine Bosgiraud, Sylvie Delebassée, Robert Granet

Publikováno v: Nucleosides and Nucleotides. 15:1849-1861

Piperazinone nucleosides can be formed by N-glycosylation with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose of either piperazin-2-ones or pyrazin-2-ones followed by reduction of the heterocycle with rhodium on alumina. All the prepared compounds

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d829f0510b8dbdcd6b85ca88f84f639e
https://doi.org/10.1080/07328319608002737

Zobrazit plný text záznamu

Synthesis and antiretroviral evaluation of 3-alkyl 2-piperazinone nucleoside analogs

Autor: Sylvie Delebassée, Abdellah Benjahad, Robert Granet, Mourad Kaouadji, R. Benhaddou, Pierre Krausz, Claudine Bosgiraud, Salomon Piekarski, François Thomasson

Publikováno v: Tetrahedron Letters. 35:9545-9548

Glycosylation of 3-alkyl N 4 -(3-hydroxypropyl) 2-piperazinones by protected 1- O -acetyl ribofuranoses produces nucleoside analogs in which the base is separated from the sugar by a hydrocarbon spacer arm. The preliminary in vitro test results again

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::53e4500c8cc51a3c4c493d8dab8bd54a
https://doi.org/10.1016/0040-4039(94)88507-9

Zobrazit plný text záznamu

Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: the nature of the C-3 substituent on anti-HIV activity

Autor: Chi Hung Nguyen, Elisabeth Thérèse Jeanne Pasquier, Dominique Jean-Pierre Mabire, Koen Andries, Jerome Emile Georges Guillemont, Abdellah Benjahad, David S. Grierson, Said Oumouch

Publikováno v: Bioorganic and medicinal chemistry letters
Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2007, 17 (3), pp.712-6. ⟨10.1016/j.bmcl.2006.10.082⟩

As part of a systematic SAR study on the 3-iodo-4-phenoxypyridinone 3 (IOPY) type non-nucleoside reverse transcriptase inhibitors, the analogues 4a-4z bearing different C-3 substituents were synthesized and evaluated for their anti-HIV activity again

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1296723f5be70151b89bd2abc69cb7e1
https://hdl.handle.net/10067/623900151162165141

Zobrazit plný text záznamu

3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

Publikováno v: Bioorganic and medicinal chemistry letters

Building upon the potent anti-HIV-1 activities observed for the 3-dimethylamino-4-benzylpyridinone 2, and the corresponding 4-aryloxypyridinone analogue 3, a concise and efficient route to the 3-iodo-4-aryloxypyridinones 14a-c (IOPY's) was developed.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfdbc1472b5b03c19bd40db14ced76bb
https://hdl.handle.net/10067/514730151162165141

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání