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Träfflista för sökning "AMNE:(MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences) ;pers:(Samuelsson Bertil)"

Sökning: AMNE:(MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences) > Samuelsson Bertil

Resultat 1-10 av 34

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Numrering	Referens	Omslagsbild	Hitta
1.	Wangsell, Fredrik, et al. (författare) Investigation of alpha-phenylnorstatine and alpha-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors 2011 Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896 .- 1464-3391. ; 19:1, s. 145-155 Tidskriftsartikel (refereegranskat)abstract Inhibition of the BACE-1 protease enzyme has over the recent decade developed into a promising drug strategy for Alzheimer therapy. In this report, more than 20 new BACE-1 protease inhibitors based on alpha-phenylnorstatine, alpha-benzylnorstatine, iso-serine, and beta-alanine moieties have been prepared. The inhibitors were synthesized by applying Fmoc solid phase methodology and evaluated for their inhibitory properties. The most potent inhibitor, tert-alcohol containing (R)-12 (IC(50) = 0.19 mu M) was co-crystallized in the active site of the BACE-1 protease, furnishing a novel binding mode in which the N-terminal amine makes a hydrogen bond to one of the catalytic aspartic acids.
2.	Ersmark, Karolina, et al. (författare) Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV 2006 Ingår i: Biorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896. ; :14, s. 2197-2208 Tidskriftsartikel (refereegranskat)
3.	Wångsell, Fredrik, et al. (författare) Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic 2009 Ingår i: Bioorganic & Medicinal Chemistry Letters. - : Elsevier. - 0960-894X .- 1464-3405. ; 19:16, s. 4711-4714 Tidskriftsartikel (refereegranskat)abstract Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC50 value of 0.23 mu M.
4.	Ersmark, Karolina, et al. (författare) Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity 2004 Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 47:1, s. 110-22 Tidskriftsartikel (refereegranskat)
5.	Johansson, Anja, et al. (författare) Tetrapeptides as potent protease inhibitors of Hepatitis C Virus full-length NS3 (protease-helicase/NTPase) 2002 Ingår i: Bioorganic & Medicinal Chemistry. - 0968-0896 .- 1464-3391. ; 10:12, s. 3915-22 Tidskriftsartikel (refereegranskat)
6.	Niklasson, Gunilla, et al. (författare) Synthesis of C-2 symmetric potential inhibitors of HIV-1 protease from D-mannitol 1996 Ingår i: Journal of carbohydrate chemistry. - : Informa UK Limited. - 0732-8303 .- 1532-2327. ; 15:5, s. 555-569 Tidskriftsartikel (refereegranskat)
7.	Nöteberg, Daniel, et al. (författare) Synthesis of enantiomerically pure cis and trans 2-aminocyclopentanecarboxylic acids. Use of proline replacements in potential HIV-protease inhibitors 1997 Ingår i: Tetrahedron. - 0040-4020 .- 1464-5416. ; 53:23, s. 7975-7984 Tidskriftsartikel (refereegranskat)abstract The synthesis of the four diastereomeric 2-aminocyclopentanecarboxylic acids, their use as replacements for proline in potential HIV protease inhibitors containing a hydroxyethylamine dipeptide isostere and the evaluation of the biological activity of these is described.
8.	Schaal, Wesley, et al. (författare) Synthesis and comperative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors 2001 Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 44:2, s. 155-169 Tidskriftsartikel (refereegranskat)
9.	Adrian Meredith, Jenny, 1971-, et al. (författare) Design and synthesis of novel P2 substituents in diol-based HIV protease inhibitors 2010 Ingår i: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 45:1, s. 160-170 Tidskriftsartikel (refereegranskat)abstract The synthesis and SAR of HIV-1 protease inhibitors containing novel P2 structural elements are presented. The inhibitors were designed having hydrogen bond accepting P2 substituents to probe potential favorable interactions to Asp-29/Asp-30 of the HIV-1 protease backbone utilizing inhibitor 3 as a model template. Several inhibitors were synthesized from an L-Val methyl amide P2 motif by appending hydrogen bonding moieties from either the isopropyl side-chain or from the methyl amide portion. The most promising inhibitors 4a and 4e displayed K-i values of 1.0 nM and 0.7 nM respectively and EC50 values in the MT4 cell-based assay of 0.17 mu M and 0.33 mu M respectively, a slight loss in potency compared to lead inhibitor 3. These inhibitors were also tested against an HIV protease inhibitor resistant strain carrying the M461, V82F, and 184V mutations. Inhibitors 4a and 4e displayed a 3 and 4 fold change respectively compared with HIV wild type, whereas lead inhibitor 3 showed a higher 9 fold change. This study further demonstrate the chemical tractability of the approach where various P2 substituents can be introduced in just one chemical step from lactone 21 enabling facile modifications of the overall properties in this inhibitor class.
10.	Adrian Meredith, Jenny, 1971-, et al. (författare) P2 '-truncated BACE-1 inhibitors with a novel hydroxethylene-like core 2010 Ingår i: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 45:2, s. 542-554 Tidskriftsartikel (refereegranskat)abstract Highly potent BACE-1 protease inhibitors derived from a novel hydroxyethylene-like core structure were recently developed by our group using X-ray crystal structure data and molecular modelling. In a continuation of this work guided by molecular modelling we have explored a truncated core motif where the P2' amide group is replaced by an ether linkage resulting in a set of alkoxy, aryloxy and alkylaryl groups, with the overall aim to reduce molecular weight and the number of amide bonds to increase permeability and bestow the inhibitors with drug-like features. The most potent of these inhibitors displayed a BACE-I IC50 value of 140 nM. The synthesis of these BACE-I inhibitors utilizes readily available starting materials, furnishing the target compounds in good overall yields.

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Resultat 1-10 av 34

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Typ av publikation: tidskriftsartikel (32); annan publikation (2)

Typ av innehåll: refereegranskat (32); övrigt vetenskapligt/konstnärligt (2)

Författare/redaktör: Samuelsson, Bert... (34)Ta bort avgränsningen; Hallberg, Anders (29); Danielson, U. Helena (12); Classon, Björn (12); Vrang, Lotta (11); Karlén, Anders (9); visa fler...; Jansson, Katarina (8); Rosenquist, Åsa (8); Kvarnström, Ingemar (7); Unge, Torsten (7); Larhed, Mats (6); Wallberg, Hans (6); Hultén, Johan (6); Hamelink, Elizabeth (6); Lindberg, Jimmy (5); Nillroth, Ulrika (5); Björklund, Catarina, ... (4); Poliakov, Anton (4); Alterman, Mathias (4); Schaal, Wesley (4); Markgren, Per-Olof (4); Danielson, Helena (3); Adolfsson, Hans (3); Adrian Meredith, Jen ... (3); Edlund, Michael (3); Oscarson, Stefan (3); Ahlsén, Göran (3); Andersson, Hans O. (3); Ayesa, Susana (3); Lindquist, Charlotta (3); Benkestock, Kurt (3); Wångsell, Fredrik (3); Pelcman, Mikael (3); Ekegren, Jenny K (3); Nilsson, Magnus (2); Agback, Tatiana (2); Winiwarter, Susanne (2); Åqvist, Johan (2); Kvarnstrom, Ingemar (2); Hämäläinen, Markku (2); Sävmarker, Jonas (2); Johansson, Anja (2); Lindeberg, Gunnar (2); Belfrage, Anna Karin (2); Lindström, Stefan (2); Åkerblom, Eva (2); Eneroth, Anders (2); Thorstensson, Fredri ... (2); Wähling, Horst (2); Rydergård, Christina (2); visa färre...

Lärosäte: Uppsala universitet (31); Stockholms universitet (10); Linköpings universitet (5); Linnéuniversitetet (1)

Språk: Engelska (34)

Forskningsämne (UKÄ/SCB): Medicin och hälsovetenskap (34); Naturvetenskap (8)

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