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pro vyhledávání: '"Alexander Minidis"'
To date, optimizing reactions let alone predicting the outcome (yield) of known reactions requires expert knowledge and can at best be obtained by computationally complex and expensive modelling. The present investigation tests if machine learning re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13d16f0f365c04d5b148974d009458b1
https://doi.org/10.26434/chemrxiv.12613214.v1
https://doi.org/10.26434/chemrxiv.12613214.v1
Autor:
Alf Claesson, Alexander Minidis
Publikováno v:
Chemical research in toxicology. 31(6)
Reactive metabolites are widely accepted as playing a pivotal role in causing idiosyncratic adverse drug reactions (IDR). However, much is unknown about the biological mechanisms of IDR, although the initiating event in most cases is an attachment of
Autor:
Nilsson Linda I, Alexander Minidis, Per I. Arvidsson, Juliette Janson, Susanne Gustavsson, Johan Lundkvist, Colin Ray, Susanne Rosqvist, Jörg Holenz, Fernando Sehgelmeble, Didier Rotticci
Publikováno v:
ChemMedChem. 7:396-399
The proof of the pudding: A proof-of-concept study using γ-secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for sulfonamides. Detailed in vitro and in vivo profiling reveal that the sulfonimidamide motif imparts de
Publikováno v:
The Journal of Organic Chemistry. 74:9328-9336
The scope and limitation of the combined ruthenium-lipase induced dynamic kinetic resolution (DKR) through O-acetylation of racemic heteroaromatic secondary alcohols, i.e., 1-heteroaryl substituted ethanols, was investigated. After initial screening
Autor:
Peter Ström, Mcleod Donald A, Anna Breitholtz-Emanuelsson, William L. Heaton, Ylva Terelius, Tao Xin, Louise Edwards, Sheehan Susan M, Keith Jarvie, Anna Nordmark, David Wensbo, Patrick Raboisson, Henrik Dahllof, Abdelmalik Slassi, Alexander Minidis, Methvin Isaac, Julie Wilson, Annika Kers
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(22)
AZD9272 and AZD6538 are two novel mGluR5 negative allosteric modulators selected for further clinical development. An initial high-throughput screening revealed leads with promising profiles, which were further optimized by minor, yet indispensable,
Autor:
Dirk Weigelt, Andreas Nolting, Karin J. Sterky, Jennie Strindlund, Fernando Sehgelmeble, Daniel Sohn, Alexander Minidis, Rebecka From, Narhi Katja, Eva Nyman, Jenny Bernström, Ellen Santangelo, Karl S. A. Vallin, Christian Linde
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(17)
A series of potent antagonists of the ion channel transient receptor potential A1 (TRPA1) was developed by modifying lead structure 16 that was discovered by high-throughput screening. Based on lead compound 16 , a SAR was established, showing a narr
Autor:
Alexander Minidis, Jan‐E. Baeckvall
Publikováno v:
ChemInform. 33
Publikováno v:
ChemInform. 33
Autor:
Alecia Peterson, David Wensbo, Andreas Wållberg, Jan P. Mattsson, Alexander Minidis, Krister Österlund, Martin Johansson, Jonas Malmström, Karolina Nilsson, Lance G. Hammerland
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(9)
Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity.
Autor:
Methvin Isaac, Stormann Thomas M, Alexander Minidis, David Wensbo, Abdelmalik Slassi, Louise Edwards, Edwin C. Johnson, Karolina Nilsson, Lance G. Hammerland, Donald McLeod, Patrick Raboisson, Jan P. Mattsson
Publikováno v:
Current topics in medicinal chemistry. 5(9)
Extensive research into the functions of glutamate and glutamate receptors in the central nervous system (CNS) has shown an essential role of metabotropic glutamate (mGlu) receptors in normal brain functions, but also in neurological and psychiatric