Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease

HIV-1 protease inhibitors continue to play an important role in the treatment of HIV/AIDS, transforming this deadly ailment into a more manageable chronic infection. Over the years, intensive research led to a variety of approved protease inhibitors for the treatment of HIV/AIDS. In this review, we outline current drug design and medicinal chemistry efforts toward the development of new generation protease inhibitors beyond the currently approved drugs.

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“…The binding affinity of both the PCU diol and PCU lactam are similarly active for the protease, though they are structurally different. 184, 185 …”

Section: (5) Recent Progress Towards Hiv-1 Protease Inhibitorsmentioning

confidence: 99%

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS

2016

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“…Molecular docking techniques have also been widely used to discover new small molecules targeting bacterial/viral proteins [8,9]. Docking is often used to predict the suitable pose and affinity of drug molecules in the binding pocket of protein targets to rationalize the active and inactive lead compounds.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

QSAR models and scaffold-based analysis of non-nucleoside HIV RT inhibitors

Nizami

Tetko

Koorbanally

et al. 2015

Chemometrics and Intelligent Laboratory Systems

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“…No significant NOE interactions were observed for the family of peptides studied herein, even at low temperature. We have successfully utilized EASY ROESY before in obtaining crucial information of the 3D solution structure of similar but different short cage peptides . This is an indication of the flexibility of AVPI peptides studied here.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and NMR elucidation of novel tetrapeptides

Makatini

Chetty

Onajole

et al. 2011

Journal of Peptide Science

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The synthesis and NMR elucidation of Ala-Val-Pro-Ile and five novel peptide-based derivatives are reported. These peptides mimic the natural second mitochondria-derived activator of caspase (Smac) protein. Purification was achieved using preparative HPLC and the NMR elucidation of all compounds is reported for the first time. A series of overlapping signals were observed in the 1D NMR spectra thus making assignment a difficult task to undertake. The use of 2D NMR techniques with the inclusion of efficient adiabatic symmetrized ROESY proved to be an effective tool in overcoming these difficulties.

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Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease

Cited by 32 publications

References 28 publications

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS

QSAR models and scaffold-based analysis of non-nucleoside HIV RT inhibitors

Synthesis and NMR elucidation of novel tetrapeptides

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