Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Carolina Martinez-Lamenca"'
Autor:
Elsie Diaz, Suraj Adhikary, Armand W. J. W. Tepper, Daniel Riley, Rodrigo Ortiz-Meoz, Daniel Krosky, Christophe Buyck, Carolina Martinez Lamenca, Josep Llaveria, Lichao Fang, Jay H. Kalin, Vincent N. A. Klaren, Shorouk Fahmy, Paul L. Shaffer, Robert Kirkpatrick, Rodrigo J. Carbajo, Maren Thomsen, Antonietta Impagliazzo
Publikováno v:
Communications Biology, Vol 5, Iss 1, Pp 1-14 (2022)
Rational engineering of human spermine oxidase yields crystallizable structures and the design of an allosteric inhibitor.
Externí odkaz:
https://doaj.org/article/391009d10cb04621862722699df90a61
Autor:
Demin Samuël Dominique, Carolina Martinez-Lamenca, Kevin Lam, Mary-Ambre Carvalho, Frederik J. R. Rombouts, Morgan Lecomte, Fedor Romanov-Michailidis
Nitriles are recurring motifs in bioactive molecules and versatile functional groups in synthetic chemistry. Despite recent progress, direct introduction of a nitrile moiety in heteroarenes remains challenging. Recent developments in electrochemical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38b9a70091dae3594763da883216d9c5
Autor:
Mary-Ambre, Carvalho, Samuël, Demin, Carolina, Martinez-Lamenca, Fedor, Romanov-Michailidis, Kevin, Lam, Frederik, Rombouts, Morgan, Lecomte
Publikováno v:
Chemistry (Weinheim an der Bergstrasse, Germany). 28(1)
Nitriles are recurring motifs in bioactive molecules and versatile functional groups in synthetic chemistry. Despite recent progress, direct introduction of a nitrile moiety in heteroarenes remains challenging. Recent developments in electrochemical
Autor:
Ann Vos, Aldo Peschiulli, Frederik J. R. Rombouts, Sven Franciscus Anna Van Brandt, Pauline Heckmann, Michel Anna Jozef De Cleyn, Solène Bache, Carolina Martinez-Lamenca, Jos Leenaerts, Harrie J.M. Gijsen, Chien-Chi Hsiao
Publikováno v:
European journal of medicinal chemistry. 228
A common challenge for medicinal chemists is to reduce the pKa of strongly basic groups' conjugate acids into a range that preserves the desired effects, usually potency and/or solubility, but avoids undesired effects like high volume of distribution
Autor:
Sergio A. Alonso de Diego, Daniel Oehlrich, Harrie J.M. Gijsen, Andrés A. Trabanco, Hana Prokopcová, Nigel Austin, Michel Surkyn, Dries Van den Bossche, Frederik J. R. Rombouts, Deborah Dhuyvetter, Gregor James Macdonald, Sven Franciscus Anna Van Brandt, Herman Borghys, Michiel Van Gool, Diederik Moechars, Aránzazu García-Molina, Michel Anna Jozef De Cleyn, Carolina Martinez-Lamenca
Publikováno v:
Journal of Medicinal Chemistry. 61:5292-5303
In previous studies, the introduction of electron withdrawing groups to 1,4-oxazine BACE1 inhibitors reduced the pKa of the amidine group, resulting in compound 2 that showed excellent in vivo efficacy, lowering Aβ levels in brain and CSF. However,
Autor:
Miranda Wright, Carolina Martinez-Lamenca, Paul Brennan, Daniel Oehlrich, Andrés A. Trabanco, Leenaerts Joseph Elisabeth
Sulfonimidamides are an emerging bioisosteric replacement in medicinal chemistry projects, and therefore new chemistries are necessary to access this functionality. The general synthesis of CF3-sulfonimidamides from an activated bench-stable transfer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0083400b4ff77f6359860609223a2db7
https://ora.ox.ac.uk/objects/uuid:c096c74e-a436-4e9c-833c-ef88627813d0
https://ora.ox.ac.uk/objects/uuid:c096c74e-a436-4e9c-833c-ef88627813d0
Autor:
Charlotte S. Richards-Taylor, Andrés A. Trabanco, Carolina Martinez-Lamenca, Leenaerts Joseph Elisabeth, Daniel Oehlrich
Publikováno v:
The Journal of organic chemistry. 82(18)
A general synthesis of CF3-sulfonimidamides from sulfinamides under both batch and continuous flow conditions is described. The reaction proceeds via a sulfonimidoyl fluoride intermediate. A reaction scope showing good group variation on the substitu
Autor:
Carolina Martinez-Lamenca, Andrés A. Trabanco, Jos Leenaerts, Sven Franciscus Anna Van Brandt, Tom R. M. Rauws, Frederik J. R. Rombouts
Publikováno v:
European Journal of Organic Chemistry. 2012:7048-7052
A simple and scalable procedure to introduce alcohols selectively at the 3-position of 3,4,5-trifluoroaniline is described. The procedure uses powdered NaOH as base and catalytic 15-crown-5 in refluxing toluene with a Dean–Stark trap. A short explo
Autor:
Carolina Martinez‐Lamenca, Chiara Zavattaro, Mirielle Braeken, Dennis Franken, Andrés A. Trabanco, Jinsheng Chen, Frederik Rombouts
Publikováno v:
Tetrahedron Letters. 51:4815-4818
A new and facile microwave-assisted protocol for the debenzylation of N-benzylamides with triflic acid has been developed. Both secondary and tertiary aliphatic or aromatic amides are obtained in moderate to good yields.
Autor:
Michiel Van Gool, Michel Surkyn, Aránzazu García-Molina, Ann Vos, Nigel Austin, Gary Tresadern, Michel Anna Jozef De Cleyn, Dieder Moechars, Carolina Martinez-Lamenca, Herman Borghys, Daniel Oehlrich, Oscar Delgado, Hana Prokopcová, Gregor James Macdonald, José Manuel Alonso, Sergio A. Alonso de Diego, Harrie J.M. Gijsen, Sven Franciscus Anna Van Brandt, Richard Alexander, Frederik J. R. Rombouts, Andrés A. Trabanco
Publikováno v:
Journal of medicinal chemistry. 58(20)
1,4-Oxazines are presented, which show good in vitro inhibition in enzymatic and cellular BACE1 assays. We describe lead optimization focused on reducing the amidine pKa while optimizing interactions in the BACE1 active site. Our strategy permitted m