Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease |
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| Authors: | Kazmierski Wieslaw M Furfine Eric Spaltenstein Andrew Wright Lois L |
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| Affiliation: | GlaxoSmithKline, Research Triangle Park, NC 27709, USA. wieslaw.m.kazmierski@gsk.com |
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| Abstract: | We have developed concise and efficient syntheses of novel spirocyclic pyrrolidones 1-3, which involve the alkylation of pyrrolidone precursor 13 with 1,5-dibromopentane, 16 and 15, followed by an in situ lactamization. Conjugates of 1 and 2 with P1'/P2' hydroxy-indanolamine moiety resulted in novel and potent inhibitors of HIV-1 protease 25 and 26, suggesting that 1 and 2 are novel P2/P1 HIV-PI mimetics. |
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