Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy

Yehia, Nasser A. M.; Antuch, Walfrido; Beck, Barbara; Hess, Sibylle; Schauer-Vukasinovic, Vesna; Almstetter, Michael; Furer, Patrick; Herdtweck, Eberhardt; Dömling, Alexander

doi:10.1016/j.bmcl.2004.04.026

Cited by 29 publications

(17 citation statements)

References 18 publications

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“…Acylated tetronic and tetramic acids have been investigated as aspartic protease inhibitors before [15] . This was due to their similarity to Tipranavir, an active site inhibitor of the HIV-1 aspartic protease.…”

Section: Introductionmentioning

confidence: 99%

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Modulators and Inhibitors of γ- and β-Secretases

Schmidt

Baumann²,

Narlawar³

et al. 2006

Neurodegener Dis

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Most gene mutations associated with Alzheimer’s disease point to the metabolism of amyloid precursor protein as a potential cause. The β- and γ-secretases are two executioners of amyloid precursor protein processing resulting in amyloid-β. Significant progress has been made in the selective inhibition of both proteases, regardless of structural information for γ-secretase. Several peptidic and nonpeptidic leads were identified for both targets.

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Section: Introductionmentioning

confidence: 99%

“…A cyclization/ cleavage strategy allowed to introduce diversity and resulted in more than 70 derivatives. The compounds [14][15][16][17] ( fig. 4 ) were tested in collaboration with F. HoffmannLa Roche, Basel, and M. Willem at the LMU, München.…”

Section: Introductionmentioning

confidence: 99%

Modulators and Inhibitors of γ- and β-Secretases

Schmidt

Baumann²,

Narlawar³

et al. 2006

Neurodegener Dis

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“…However, while inherently structurally diverse, it is evident from the representative structures 188-190 that this series exhibits only modest inhibitory potency with IC 50 values ranging from 1−>1000 µM [495].…”

Section: Hiv Protease Inhibitors (Hiv Pis)mentioning

confidence: 98%

“…Non-peptidic inhibitors of HIV protease were explored using a novel multi-component chemistry strategy that produced a series 3-hydroxy-5-oxo-2,5-dihydrofuran-2-carboxamide derivatives in which the core element is substituted with three groups designed to provide four projections into the S2'/S1' and S1/S2 binding pockets [495]. However, while inherently structurally diverse, it is evident from the representative structures 188-190 that this series exhibits only modest inhibitory potency with IC 50 values ranging from 1−>1000 µM [495].…”

Section: Hiv Protease Inhibitors (Hiv Pis)mentioning

confidence: 99%

Developments in Antiviral Drug Design, Discovery and Development in 2004

Meanwell

Belema²,

Carini³

et al. 2005

CDTID

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This article summarizes key aspects of progress made during 2004 toward the design, discovery and development of antiviral agents for clinical use. Important developments in the identification, characterization and clinical utility of inhibitors of human immunodeficiency virus; the hepatitis viruses, hepatitis B, hepatitis C; the herpes family of viruses, herpes simplex viruses 1 and 2, varicella zoster virus, Epstein-Barr virus and human cytomegalovirus; the respiratory viruses, influenza, respiratory syncytial virus, human metapneumovirus, picornaviruses, measles and the severe acute respiratory syndrome coronavirus; human papilloma virus; rotavirus; Ebola virus and West Nile virus, are reviewed.

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“…Researchers from Hoffmann-La Roche described a broad series of tetronic and tetramic acids with BACE inhibitor [104]. Acylated tetronic and tetramic acids have been investigated as aspartic protease inhibitors before [105]. This was due to their similarity to Tipranavir, an active site inhibitor of the HIV-1 aspartic protease.…”

Section: Bace Inhibitorsmentioning

confidence: 99%

Inhibitors and Modulators of β- and γ-Secretase

Schmidt

Baumann²,

Braun³

et al. 2006

CTMC

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Most gene mutations associated with Alzheimer's disease point to the metabolism of amyloid precursor protein as potential cause. The beta- and gamma-secretases are two executioners of amyloid precursor protein processing resulting in amyloid beta. Significant progress has been made in the selective inhibition of both proteases, regardless of structural information for gamma-secretase. Several peptidic and non-peptidic leads were identified and first drug candidates are in clinical trials. This review focuses on the developments since 2003.

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Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy

Cited by 29 publications

References 18 publications

Modulators and Inhibitors of γ- and β-Secretases

Modulators and Inhibitors of γ- and β-Secretases

Developments in Antiviral Drug Design, Discovery and Development in 2004

Inhibitors and Modulators of β- and γ-Secretase

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Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy

Cited by 29 publications

References 18 publications

Modulators and Inhibitors of γ- and β-Secretases

Modulators and Inhibitors of γ- and β-Secretases

Developments in Antiviral Drug Design, Discovery and Development in 2004

Inhibitors and Modulators of &#946;- and &#947;-Secretase

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Inhibitors and Modulators of β- and γ-Secretase