Výsledky vyhledávání - "Ingemar Kvarnström"

Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes

Autor: Jimmy Lindberg, Veronica Sandgren, Per-Ola Johansson, Bertil Samuelsson, Tatiana Agback, Oscar Belda, Anders Dahlgren, Ingemar Kvarnström

Publikováno v: Bioorganic & Medicinal Chemistry. 20:4377-4389

A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18d5fc4bd480a7a3d040ed0dfd1b0c8a
https://doi.org/10.1016/j.bmc.2012.05.039

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Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core

Autor: Karin Gustafsson, Jimmy Lindberg, Ingemar Kvarnström, Bertil Samuelsson, Fredrik Wångsell, Anders Hallberg, Åsa Rosenquist, Katarina Jansson, Neera Borkakoti, Michael Edlund

Publikováno v: European Journal of Medicinal Chemistry. 45:870-882

We herein describe the design and synthesis of a series of BACE-1 inhibitors incorporating a P1-substituted hydroxylethylene transition state isostere. The synthetic route starting from commercially available carbohydrates yielded a pivotal lactone i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::475d8ec9cdeac6a6b4f84dd45d430a09
https://doi.org/10.1016/j.ejmech.2009.11.013

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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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Potent inhibitors of the hepatitis C virus NS3 protease: Use of a novel P2 cyclopentane-derived template

Autor: Elizabeth Hamelink, Åsa Rosenquist, Lotta Vrang, Bertil Samuelsson, Marcus Bäck, Katarina Jansson, Ingemar Kvarnström, Anders Hallberg, Per-Ola Johansson

Publikováno v: Bioorganic & Medicinal Chemistry. 14:5136-5151

The HCV NS3 protease is essential for replication of the hepatitis C virus (HCV) and therefore constitutes a promising new drug target for anti-HCV therapy. Several potent and promising HCV NS3 protease inhibitors, some of which display low nanomolar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48e05a109d7d58eb99ce5cfd5c1e5743
https://doi.org/10.1016/j.bmc.2006.04.008

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Design and Synthesis of Potent Inhibitors of Plasmepsin I and II: X-ray Crystal Structure of Inhibitor in Complex with Plasmepsin II

Autor: Lotta Vrang, Ingemar Kvarnström, Bertil Samuelsson, Anders Hallberg, Jimmy Lindberg, Elizabeth Hamelink, Åsa Rosenquist, Michael J. Blackman, Per-Ola Johansson

Publikováno v: Journal of Medicinal Chemistry. 48:4400-4409

New and potent inhibitors of the malarial aspartic proteases plasmepsin (Plm) I and II, from the deadliest malaria parasite Plasmodium falciparum, have been synthesized utilizing Suzuki coupling reactions on previously synthesized bromobenzyloxy-subs

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::189d8ae12116ac1d45594c7ebea5bccd
https://doi.org/10.1021/jm040884n

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Design and Synthesis of Potent Inhibitors of the Malaria Aspartyl Proteases Plasmepsin I and II. Use of Solid-Phase Synthesis to Explore Novel Statine Motifs

Autor: Per-Ola Johansson, Katarina Jansson, Lotta Vrang, Yantao Chen, Anna Karin Gertrud Linnea Belfrage, Anders Hallberg, Bertil Samuelsson, Åsa Rosenquist, Ingemar Kvarnström, Elizabeth Hamelink, Michael J. Blackman

Publikováno v: Journal of Medicinal Chemistry. 47:3353-3366

Picomolar to low nanomolar inhibitors of the two aspartic proteases plasmepsin (Plm) I and II, from the malaria parasite Plasmodium falciparum, have been identified from sets of libraries containing novel statine-like templates modified at the amino

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad85ebf0ea8227fc3c032bdf548cf28f
https://doi.org/10.1021/jm031106i

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New inhibitors of the malaria aspartyl proteases plasmepsin I and II

Autor: Anders Hallberg, Anders Dahlgren, Ingemar Kvarnström, Bertil Samuelsson, Lotta Vrang, Åsa Rosenquist, Elizabeth Hamelink

Publikováno v: Bioorganic & Medicinal Chemistry. 11:3423-3437

New inhibitors of plasmepsin I and II, the aspartic proteases of the malaria parasite Plasmodium falciparum, are described. From paralell solution phase chemistry, several reversed-statine type isostere inhibitors, many of which are aza-peptides, hav

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9cbc92849e6344108b56eb6b44cfd169
https://doi.org/10.1016/s0968-0896(03)00312-2

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Solid-phase library synthesis of reversed-statine type inhibitors of the malarial aspartyl proteases plasmepsin I and II

Autor: Anders Hallberg, Anders Dahlgren, Lotta Vrang, Ingemar Kvarnström, Bertil Samuelsson, Åsa Rosenquist, Elizabeth Hamelink

Publikováno v: Bioorganic & Medicinal Chemistry. 11:827-841

With the aim to develop inhibitors of the plasmepsin I and II aspartic proteases of the malaria parasite Plasmodium falciparum, we have synthesized sets of libraries from novel reversed-statine isosteres, using a combination of solution phase and sol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd7a2858fa6681b6914c721dd464b6b0
https://doi.org/10.1016/s0968-0896(02)00568-0

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Novel Morpholinone-Based ?-Phe-Pro-Arg Mimics as Potential Thrombin Inhibitors: Design, Synthesis, and X-ray Crystal Structure of an Enzyme Inhibitor Complex

Autor: Anders Dahlgren, Per Johansson, Ingemar Kvarnström, Djordje Musil, Ingemar Nilsson, Bertil Samuelsson

Publikováno v: Bioorganic & Medicinal Chemistry. 10:1829-1839

A morpholinone structural motif derived from D(+)- and L(-)-malic acid has been used as a mimic of D-Phe-Pro in the thrombin inhibiting tripeptide D-Phe-Pro-Arg. In place of Arg the more rigid P1 truncated p-amidinobenzylamine (Pab) or 2-amino-5-amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1980cb69353304c0d0aac2df246bf2a4
https://doi.org/10.1016/s0968-0896(02)00023-8

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Synthesis of Potential Thrombin Inhibitors. Incorporation of Tartaric Acid Templates as P2 Proline Mimetics

Autor: Jonas Brånalt, Anders Dahlgren, Ingemar Nilsson, Djordje Musil, Bertil Samuelsson, Ingemar Kvarnström

Publikováno v: Bioorganic & Medicinal Chemistry. 10:1567-1580

With the objective to prepare novel non-peptidic thrombin inhibitors, bioisosteres of the inhibitory tripeptide D-Phe-Pro-Arg chain have been examined. Thus, the P1 Arg was replaced with p-amidinobenzylamine, an elongated homologue of the same and wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d242f307ad9430729ed7b52840e5d088
https://doi.org/10.1016/s0968-0896(01)00426-6

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