Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand

N M Patel; F Bennett; V M Girijavallabhan; B Dasmahapatra; N Butkiewicz; A Hart

doi:10.1016/s0960-894x(98)00144-9

Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand

Bioorg Med Chem Lett. 1998 Apr 21;8(8):931-4. doi: 10.1016/s0960-894x(98)00144-9.

Authors

N M Patel¹, F Bennett, V M Girijavallabhan, B Dasmahapatra, N Butkiewicz, A Hart

Affiliation

¹ Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.

PMID: 9871514
DOI: 10.1016/s0960-894x(98)00144-9

Abstract

Studies involving modifications to the P3 position of previously described HIV-protease inhibitors containing beta-hydroxyether and thioether dipeptide isostere replacements led to the discovery of pseudopeptides 8o and 8p with improved antiviral activities.

MeSH terms

Dipeptides / chemical synthesis*
Dipeptides / chemistry
Dipeptides / pharmacology
Ethers
HIV / drug effects*
HIV Protease Inhibitors / chemical synthesis*
HIV Protease Inhibitors / chemistry
HIV Protease Inhibitors / pharmacology
Microbial Sensitivity Tests
Molecular Conformation
Molecular Structure
Stereoisomerism
Structure-Activity Relationship

Substances

Dipeptides
Ethers
HIV Protease Inhibitors