Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 23, Pages 3431-3433Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00733-3
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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 HTV-1 protease 25 and 26. suggesting that 1 and 2 are novel P2/P1 HIV-P1 mimetics. (C) 2002 Elsevier Science Ltd. All rights reserved.
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