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

DOI: 10.1016/0960-894X(96)00468-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2531 - 2536 (1996)

Update date:2022-08-05

Topics:

Authors:

Abbenante

Bergman Bergman

Brinkworth

March March

Reid Reid

Hunt Hunt

James James

Dancer Dancer

Garnham Garnham

Stoermer

Fairlie Fairlie

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Article abstract of DOI:10.1016/0960-894X(96)00468-4

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.

Full text of DOI:10.1016/0960-894X(96)00468-4

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