Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones
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.
Boros, Eric E.,Johns, Brian A.,Garvey, Edward P.,Koble, Cecilia S.,Miller, Wayne H.
p. 5668 - 5672
(2007/10/03)
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