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Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease

✍ Scribed by G. Abbenante; D.A. Bergman; R.I. Brinkworth; D.R. March; R.C. Reid; P.A. Hunt; I.W. James; R.J. Dancer; B. Garnham; M.L. Stoermer; D.P. Fairlie

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 261 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00468-4

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✦ Synopsis

A series of appended macrocycles were synthesized and tested as inhibitors of HIV-1 protease (HIV PR). The macrocycle structurally mimics an N-terminal tripeptide component of peptide substrates. Structure-activity relationships explore steric limitations to the size and shape of the substituents and provide evidence for functional mimicry of substrate components.

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