Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones |
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| Authors: | Boros Eric E Johns Brian A Garvey Edward P Koble Cecilia S Miller Wayne H |
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| Affiliation: | GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA. eric.e.boros@gsk.com |
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| Abstract: | An efficient synthesis of methyl 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-one-6-carboxylates (8-10 and 16) and 6-carboxamides (17-20) is described. Sub-micromolar enzyme inhibition of HIV integrase was achieved with several carboxamide analogs which were superior to their carboxylic ester congeners. |
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