دورية أكاديمية
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
| العنوان: | Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents. |
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| المؤلفون: | Guillemont J; Medicinal Chemistry Department, TIBOTEC, Campus de Maigremont BP315, 27430 Val de Reuil, France. ,jguillem@its.jnj.com, Benjahad A, Oumouch S, Decrane L, Palandjian P, Vernier D, Queguiner L, Andries K, de Béthune MP, Hertogs K, Grierson DS, Nguyen CH |
| المصدر: | Journal of medicinal chemistry [J Med Chem] 2009 Dec 10; Vol. 52 (23), pp. 7473-87. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Washington Dc : American Chemical Society Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- |
| مواضيع طبية MeSH: | Anti-HIV Agents/*chemical synthesis , Anti-HIV Agents/*pharmacology , HIV/*drug effects , Iodopyridones/*chemical synthesis , Iodopyridones/*pharmacology, Anti-HIV Agents/chemistry ; Cell Line ; HIV/enzymology ; HIV/genetics ; HIV Reverse Transcriptase/antagonists & inhibitors ; HIV Reverse Transcriptase/genetics ; Humans ; Inhibitory Concentration 50 ; Iodopyridones/chemistry ; Mutation ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology |
| مستخلص: | 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 use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase inhibitory properties, for example, compounds 93 and 99 are active at 0.6-50 nM against wild type HIV-1 and a panel of major simple/double HIV mutant strains. |
| المشرفين على المادة: | 0 (Anti-HIV Agents) 0 (Iodopyridones) 0 (Small Molecule Libraries) EC 2.7.7.49 (HIV Reverse Transcriptase) |
| تواريخ الأحداث: | Date Created: 20090804 Date Completed: 20091231 Latest Revision: 20091203 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1021/jm900802y |
| PMID: | 19645483 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1520-4804 |
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| DOI: | 10.1021/jm900802y |