Literature DB >> 10866371

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.

A Spaltenstein1, M R Almond, W J Bock, D G Cleary, E S Furfine, R J Hazen, W M Kazmierski, F G Salituro, R D Tung, L L Wright.   

Abstract

A novel series of HIV protease inhibitors containing cyclic P1/P2 scaffolds has been synthesized and evaluated for biological activity. The trans 3,5-dibenzyl-2-oxo pyrrolidinone ring system resulted in a 50 pM enzyme inhibitor against HIV protease in vitro when combined with an indanolamine derived P'-backbone. This compound also shows comparable activity to currently marketed drugs in the MT-4 cell-based antiviral assay.

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Year:  2000        PMID： 10866371

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  12 in total

1.  4-Amino-2,3-dihydro-1λ6-isothiazole-1,1-dioxides and their chemical properties evaluation.

Authors:  Maksim S Dyachenko; Alexey V Dobrydnev; Yulian M Volovenko
Journal:  Mol Divers       Date:  2018-06-28       Impact factor: 2.943

2.  Gold(I)-Catalyzed Intramolecular Hydroamination of N-Allylic,N'-Aryl Ureas to form Imidazolidin-2-ones.

Authors:  Hao Li; Feijie Song; Ross A Widenhoefer
Journal:  Adv Synth Catal       Date:  2011-04-18       Impact factor: 5.837

3.  Intracellular antiviral activity of low-dose ritonavir in boosted protease inhibitor regimens.

Authors:  Amedeo De Nicolò; Marco Simiele; Andrea Calcagno; Adnan Mohamed Abdi; Stefano Bonora; Giovanni Di Perri; Antonio D'Avolio
Journal:  Antimicrob Agents Chemother       Date:  2014-05-05       Impact factor: 5.191

4.  Asymmetric Palladium-Catalyzed Alkene Carboamination Reactions for the Synthesis of Cyclic Sulfamides.

Authors:  Zachary J Garlets; Kaia R Parenti; John P Wolfe
Journal:  Chemistry       Date:  2016-03-10       Impact factor: 5.236

5.  Influence of catalyst structure and reaction conditions on anti- versus syn-aminopalladation pathways in Pd-catalyzed alkene carboamination reactions of N-allylsulfamides.

Authors:  Ryan M Fornwald; Jonathan A Fritz; John P Wolfe
Journal:  Chemistry       Date:  2014-06-17       Impact factor: 5.236

6.  Gold(I)-catalyzed intramolecular dihydroamination of allenes with N,N'-disubstituted ureas to form bicyclic imidazolidin-2-ones.

Authors:  Hao Li; Ross A Widenhoefer
Journal:  Org Lett       Date:  2009-06-18       Impact factor: 6.005

7.  P2' benzene carboxylic acid moiety is associated with decrease in cellular uptake: evaluation of novel nonpeptidic HIV-1 protease inhibitors containing P2 bis-tetrahydrofuran moiety.

Authors:  Ravikiran S Yedidi; Kenji Maeda; W Sean Fyvie; Melinda Steffey; David A Davis; Ira Palmer; Manabu Aoki; Joshua D Kaufman; Stephen J Stahl; Harisha Garimella; Debananda Das; Paul T Wingfield; Arun K Ghosh; Hiroaki Mitsuya
Journal:  Antimicrob Agents Chemother       Date:  2013-07-22       Impact factor: 5.191

8.  Efficient synthesis of gamma-lactams by a tandem reductive amination/lactamization sequence.

Authors:  Julica Nöth; Kevin J Frankowski; Benjamin Neuenswander; Jeffrey Aubé; Oliver Reiser
Journal:  J Comb Chem       Date:  2008-03-14

9.  Stereoselective synthesis of imidazolidin-2-ones via Pd-catalyzed alkene carboamination. Scope and limitations.

Authors:  Jonathan A Fritz; John P Wolfe
Journal:  Tetrahedron       Date:  2008       Impact factor: 2.457

10.  Stereocontrolled synthesis of bicyclic ureas and sulfamides via Pd-catalyzed alkene carboamination reactions.

Authors:  Nicholas R Babij; Jordan R Boothe; Grace M McKenna; Ryan M Fornwald; John P Wolfe
Journal:  Tetrahedron       Date:  2019-04-20       Impact factor: 2.457
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