Výsledky vyhledávání - "Hans Wallberg"

Design and Synthesis of P1–P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors

Autor: Hans Wallberg, Mats Larhed, Anders Hallberg, Johan Unge, Jean-Baptiste Veron, Bertil Samuelsson, Advait Arun Joshi, Åsa Rosenquist

Publikováno v: Journal of Medicinal Chemistry. 56:8999-9007

To study P1-P3 macrocyclizations of previously reported tertiary-alcohol-comprising HIV-1 protease inhibitors (PIs), three new 14- and 15-member macrocyclic PIs were designed, synthesized by ring-closing metathesis, and evaluated alongside with 10 no

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce6fc17f6916252a2c3fa2f6d2bc2df2
https://doi.org/10.1021/jm400811d

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Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors

Autor: Johan Unge, Alejandro Trejos, Xiongyu Wu, Mats Larhed, Per Öhrngren, Lotta Vrang, Åsa Rosenquist, Advait Arun Joshi, Magnus Persson, Hans Wallberg, Riina K. Arvela, Bertil Samuelsson

Publikováno v: Journal of Medicinal Chemistry

In an effort to identify a new class of druglike HIV-1 protease inhibitors, four different stereopure β-hydroxy γ-lactam-containing inhibitors have been synthesized, biologically evaluated, and cocrystallized. The impact of the tether length of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8e08f363ec392aa48e91c23e6a9917f
http://europepmc.org/articles/PMC3310203

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Synthesis of the Hepatitis B Nucleoside Analogue Lagociclovir Valactate

Autor: Karol Horvath, Martin Brodszki, Hans Wallberg, Horst Wähling, Håkan Malmgren, Mikael Pelcman, Birthe Bäckström, Torbjörn Larsson, Johan Wennerberg

Publikováno v: Organic Process Research & Development. 15:1027-1032

2′,3′-Dideoxy-3′-fluoro-5-O-[(S)-(+)-2-(l-valyloxy)-propionyl] guanosine (lagociclovir valactate) is a prodrug of 3′-fluoro-2′,3′-dideoxyguanosine with high oral bioavailability in humans and potent activity against hepatitis B virus (HBV

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5fdc049514fe324c6f2438073c661874
https://doi.org/10.1021/op200153s

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HIV-1 Protease Inhibitors with a Transition-State Mimic Comprising a Tertiary Alcohol: Improved Antiviral Activity in Cells

Autor: Bertil Samuelsson, Jenny K. Ekegren, Mats Larhed, Linda Axelsson, Hans Wallberg, Jacob Kihlström, Anders Hallberg, Johan Wannberg, Torsten Unge, A. K. Mahalingam

Publikováno v: Journal of Medicinal Chemistry. 53:607-615

By a small modification in the core structure of the previously reported series of HIV-1 protease inhibitors that encompasses a tertiary alcohol as part of the transition-state mimicking scaffold, up to 56 times more potent compounds were obtained ex

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::767caf1d50231e6a2eba407b205783f0
https://doi.org/10.1021/jm901165g

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Does a Fast Nuclear Magnetic Resonance Spectroscopy- and X-Ray Crystallography Hybrid Approach Provide Reliable Structural Information of Ligand-Protein Complexes? A Case Study of Metalloproteinases

Autor: Helena Kovacs, Tatiana Agback, Claudio Luchinat, Andrea Giachetti, Susanne Nyström, Dean Derbyshire, Hans Wallberg, Ivano Bertini, Johan Isaksson

Publikováno v: Journal of Medicinal Chemistry. 52:1712-1722

A human matrix metalloproteinase (MMP) hydroxamic acid inhibitor (CGS27023A) was cross-docked into 15 MMP-12, MMP-13, MMP-9, and MMP-1 cocrystal structures. The aim was to validate a fast protocol for ligand binding conformation elucidation and to pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05054b9400ae9afbffd046e0bb9489e7
https://doi.org/10.1021/jm801388q

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Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: Use of cyclopentane and cyclopentene P2-motifs

Autor: Christina Rydergård, Hans Wallberg, Björn Classon, Åsa Rosenquist, Stefan Lindström, Elizabeth Hamelink, Per-Ola Johansson, Bertil Samuelsson, Ingemar Kvarnström, Fredrik Thorstensson, Susana Ayesa, Anders Hallberg, Fredrik Wångsell, Mikael Pelcman, Horst Wähling, Marcus Bäck, Katarina Jansson, Lotta Vrang

Publikováno v: Bioorganic & Medicinal Chemistry. 15:7184-7202

Several highly potent novel HCV NS3 protease inhibitors have been developed from two inhibitor series containing either a P2 trisubstituted macrocyclic cyclopentane- or a P2 cyclopentene dicarboxylic acid moiety as surrogates for the widely used N-ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15921dd4d5e74960f57d655a5ff961ae
https://doi.org/10.1016/j.bmc.2007.07.027

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A New Class of HIV-1 Protease Inhibitors Containing a Tertiary Alcohol in the Transition-State Mimicking Scaffold

Autor: Mayada Zreik Safa, Torsten Unge, Jenny K. Ekegren, Hans Wallberg, Anders Hallberg, Bertil Samuelsson

Publikováno v: Journal of Medicinal Chemistry. 48:8098-8102

Novel HIV-1 protease inhibitors encompassing a tertiary alcohol as part of the transition-state mimicking unit have been synthesized. Variation of the P1'-P3' residues and alteration of the tertiary alcohol absolute stereochemistry afforded 10 inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70d83217646dbf3e59f9d65938d1e16c
https://doi.org/10.1021/jm050790t

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