Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Gergely M. Makara"'
Publikováno v:
ACS Medicinal Chemistry Letters. 12:185-194
Molecular design is of utmost importance in lead optimization programs ultimately determining the fate of the project and the speed to reach preclinical stage. Newly designed lead analogues or new chemotypes must successfully address the challenges i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ebbb40867ad712077199c807dea439b6
https://doi.org/10.1021/acsmedchemlett.0c00540
https://doi.org/10.1021/acsmedchemlett.0c00540
Publikováno v:
ACS Med Chem Lett
[Image: see text] Molecular design is of utmost importance in lead optimization programs ultimately determining the fate of the project and the speed to reach preclinical stage. Newly designed lead analogues or new chemotypes must successfully addres
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b9f69ac71c10d5c721be2947aa23250d
https://pubmed.ncbi.nlm.nih.gov/33603964
https://pubmed.ncbi.nlm.nih.gov/33603964
Publikováno v:
Der Pharmacia Sinica. 10
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b3e26415d4f2d3aa58b7ad3dd2b91444
https://doi.org/10.21767/0976-8688-c1-002
https://doi.org/10.21767/0976-8688-c1-002
Autor:
Tamás Sipőcz, László Lengyel, Gergely M. Makara, Teréz Vágó, János Gerencsér, Gellért Sipos, Ferenc Darvas, György Dormán
Publikováno v:
Organic Process Research & Development. 19:399-409
In the present paper we report the synthesis of condensed pyrimidone heterocycles (including novel ones) prepared by the Gould–Jacobs reaction using an in-house-built vacuum-to-high pressure multipurpose “three-mode” pyrolysis reactor. Four of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::89e9ac7ada52e9ce454a0a362bbf4c01
https://doi.org/10.1021/op500354z
https://doi.org/10.1021/op500354z
Autor:
Kristian K. Jensen, Qi Luo, Ming-juan Luo, Neil S. Geoghagen, Yusheng Xiong, Gergely M. Makara, Claude Dufresne, William A. LaMarr, Bernard K. Choi, Lorraine Malkowitz, Can C. Ozbal, Tom G. Holt
Publikováno v:
ASSAY and Drug Development Technologies. 7:495-506
Label-free mass spectrometric (MS) technologies are particularly useful for enzyme assay design for drug discovery screens. MS permits the selective detection of enzyme substrates or products in a wide range of biological matrices without need for de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8b0571df79ecb033a4dddc38b81d659
https://doi.org/10.1089/adt.2009.0200
https://doi.org/10.1089/adt.2009.0200
Autor:
György M. Keserü, Gergely M. Makara
Publikováno v:
Nature Reviews Drug Discovery. 8:203-212
By analysing the physicochemical properties of a database of hits and leads, Keseru and Makara conclude that high-throughput screening, as well as hit-to-lead optimization practices in general, are responsible for the unfavourable physicochemical pro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0a076c632ec00a768a49f4078e61bc7d
https://doi.org/10.1038/nrd2796
https://doi.org/10.1038/nrd2796
Autor:
Threshia S. Malcolm, Ping Lan, Benjamin D. Stevens, F. Anthony Romero, Dariusz Wodka, Gergely M. Makara
Publikováno v:
Tetrahedron Letters. 49:1910-1914
An expeditious method to access 2-substituted benzimidazoles was developed. Both aromatic (phenols, anilines, and thiophenols) and alkyl nucleophiles (amines and thiols) react with 2-methylsulfonyl benzimidazole under solvent-free conditions to gener
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f2a4ceeff2e95857a9c32903c2353518
https://doi.org/10.1016/j.tetlet.2008.01.100
https://doi.org/10.1016/j.tetlet.2008.01.100
Autor:
Gergely M. Makara
Publikováno v:
Journal of Medicinal Chemistry. 50:3214-3221
Fragment-based lead discovery has over the years matured into an attractive alternative to high-throughput screening (HTS) for lead generation. Several techniques for screening libraries of typically 10(3)-10(4) fragments have been reported. In this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e08328579d375e8b0330cc6caf6f3545
https://doi.org/10.1021/jm0700316
https://doi.org/10.1021/jm0700316
Autor:
Gyoergy Dorman, Gergely M. Makara, János Gerencsér, László Lengyel, Teréz Vágó, Tamas Sipocz, Gellért Sipos, Ferenc Darvas
Publikováno v:
ChemInform. 46
The synthesis of a series of fused pyrimidine heterocycles (including some novel ones) via Gould-Jacobs reactions using an in-house-built vacuum-to-high pressure multipurpose pyrolysis reactor is described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9b08eba7688c325e73b156767757cf2a
https://doi.org/10.1002/chin.201535196
https://doi.org/10.1002/chin.201535196
Autor:
John Athanasopoulos, Gergely M. Makara
Publikováno v:
Current Opinion in Biotechnology
Affinity technologies have been applied at several stages of the drug discovery process, ranging from target identification and purification to the identification of preclinical candidates. The detection of ligand–macromolecule interactions in lead
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::188d7bc40d98e971d7850732708566f4
http://europepmc.org/articles/PMC7126921
http://europepmc.org/articles/PMC7126921