Journal ArticleDOI
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease
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TLDR
Compounds of a combinatorial monocyclic beta-lactam library were found to be apparently uncompetitive inhibitors of HIV-1 protease, providing lead compounds for a new class of HIV protease inhibitors.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2005-06-15. It has received 134 citations till now. The article focuses on the topics: HIV-1 protease & HIV Protease Inhibitor.read more
Citations
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Isocyanide-based multicomponent reactions in drug discovery.
TL;DR: This review describes recent advances in the application of isocyanide-based multicomponent reactions (IMCRs) in drug discovery and summarizes the various chemotypes used to probe biological targets.
Journal ArticleDOI
Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics
TL;DR: This review describes the developments since 2002 of IMCRs-cyclization strategies towards a wide variety of small cyclic mimics, medium sized cyclic constructs and macrocyclic peptidomimetics.
Journal ArticleDOI
The enzymes of β-lactam biosynthesis
Refaat B. Hamed,Gomez-Castellanos,Luc Henry,Christian Ducho,Michael A. McDonough,Christopher J. Schofield +5 more
TL;DR: This work reviews knowledge of the pathways leading to β-lactam antibiotics focusing on the mechanisms, structures and biocatalytic applications of the enzymes involved.
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2-Azetidinone--a new profile of various pharmacological activities
TL;DR: The present review article focuses on the pharmacological profile of 2-azetidinones with their potential activities.
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Synthesis and antimicrobial activity of β-lactam-bile acid conjugates linked via triazole
Namdev S. Vatmurge,Braja G. Hazra,Vandana S. Pore,Fazal Shirazi,Pradnya S. Chavan,Mukund V. Deshpande +5 more
TL;DR: Novel 1,2,3-triazole-linked beta-lactam-bile acid conjugates 17-24 and most of the compounds exhibited significant antifungal and moderate antibacterial activity against all the tested strains.
References
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Journal ArticleDOI
Comparison of the HIV‐1 and HIV‐2 proteinases using oligopeptide substrates representing cleavage sites in Gag and Gag‐Pol polyproteins
TL;DR: The substrate specificity of the human immunodeficiency virus type 1 (HIV‐1) and type 2 (Hiv‐2) proteinases was compared using oligopeptides corresponding to cleavage sites in the Gag and Gag‐Pol polyproteins of both viruses.
Journal ArticleDOI
Stability and activity of human immunodeficiency virus protease: comparison of the natural dimer with a homologous, single-chain tethered dimer
TL;DR: A tethered dimer of human immunodeficiency virus protease (HIV-PR) was produced by expression of a synthetic gene in Escherichia coli.
Journal ArticleDOI
Peptidomimetic Inhibitors of HIV Protease
John T. Randolph,David A. Degoey +1 more
TL;DR: An overview of the discovery and clinical trials of the currently approved HIV protease inhibitors is provided, followed by an examination of important aspects of therapy, such as pharmacokinetic enhancement, resistance and side effects.
Journal ArticleDOI
The inhibition of human immunodeficiency virus proteases by ‘interface peptides’
Hans J. Schramm,Joachim Boetzel,Jochen Büttner,Erich Fritsche,Walter Göhring,Ernst Jaeger,Stephan König,Oliver Thumfart,Traudl Wenger,Norbert E. Nagel,Wolfgang Schramm +10 more
TL;DR: Kinetic studies confirmed the 'dissociative' mechanism of inhibition by the peptides and both dimerization inhibition and competitive inhibition were observed, as well as synergistic effects between competitive inhibitors and interface peptides.
Journal ArticleDOI
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
James C. Sutton,Scott A. Bolton,Malcolm E. Davis,Karen S. Hartl,Bruce L. Jacobson,Arvind Mathur,Martin L. Ogletree,William A. Slusarchyk,Robert Zahler,Steven M. Seiler,Gregory S. Bisacchi +10 more
TL;DR: A series of nonguanidine N 1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group and potent inhibitors with improved specificity were discovered.
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