Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Amelie L. Bartuschat"'
Autor:
Oliver Fischer, Markus R. Heinrich, Josefa Hofmann, Martin F. Fromm, Hannelore Rampp, Gerald Pratsch, Peter Gmeiner, Regina Verena Taudte, Harald Hübner, Amelie L. Bartuschat, Jonas Kaindl
Publikováno v:
Journal of medicinal chemistry. 63(8)
Muscarinic M3 receptor antagonists and inverse agonists displaying high affinity and subtype selectivity over the antitarget M2 are valuable pharmacological tools and may enable improved treatment of chronic obstructive pulmonary disease (COPD), asth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5526e34bb7c2fcf85261b41b36e024d8
https://pubmed.ncbi.nlm.nih.gov/32202101
https://pubmed.ncbi.nlm.nih.gov/32202101
Autor:
Hannelore Rampp, Markus R. Heinrich, Xiangyu Liu, Katrin Eitel, Inbar Fish, Peter Gmeiner, Sandra G. Vincent, Roger K. Sunahara, Ashutosh Banerjee, Hongtao Liu, Harald Hübner, Josefa Hofmann, Mary J. Clark, Brian K. Kobilka, Kunio Hirata, Amelie L. Bartuschat, John T. Fisher, Brian K. Shoichet, Jonas Kaindl, Benjamin Schaake
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America, vol 115, iss 47
Liu, Hongtao; Hofmann, Josefa; Fish, Inbar; Schaake, Benjamin; Eitel, Katrin; Bartuschat, Amelie; et al.(2018). Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 115(47), 12046-12050. doi: 10.1073/pnas.1813988115. UC San Diego: Retrieved from: http://www.escholarship.org/uc/item/7dq0974t
Proceedings of the National Academy of Sciences of the United States of America
Liu, Hongtao; Hofmann, Josefa; Fish, Inbar; Schaake, Benjamin; Eitel, Katrin; Bartuschat, Amelie; et al.(2018). Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 115(47), 12046-12050. doi: 10.1073/pnas.1813988115. UC San Diego: Retrieved from: http://www.escholarship.org/uc/item/7dq0974t
Proceedings of the National Academy of Sciences of the United States of America
Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes. Starting from a single amino acid difference in the orthosteric pockets in M
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81e6552391e24497b235d3deddc51c2d
https://doi.org/10.1073/pnas.1813988115
https://doi.org/10.1073/pnas.1813988115
Publikováno v:
Synthesis. 51:976-984
The proline derivatives (2S,5S)dmamPro, (2S,5S)N-Boc-amPro and (2R,5R)dmamPro are useful building blocks for peptides since they allow conformational fixation of peptidyl–CO–N-prolyl bonds in the unusual cis conformation. The stereoselective synt
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e961eee1a540f2cef1620c39651b41b3
https://doi.org/10.1055/s-0037-1610304
https://doi.org/10.1055/s-0037-1610304
Publikováno v:
Angewandte Chemie. 127:10433-10437
Tertiare Amide, die ublicherweise als cis-trans-Gemische auftreten, konnen wirkungsvoll in die cis-Konformation uberfuhrt werden, indem man eine positive Ladung in der Nahe der Amidcarbonylgruppe platziert. Dieser Effekt ermoglichte die Herstellung e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f820c79f41985c5c4ffa0d695e879f7
https://doi.org/10.1002/ange.201502474
https://doi.org/10.1002/ange.201502474
Publikováno v:
Bioorganic & Medicinal Chemistry. 23:3938-3947
Phenylazocarboxamides can serve as bioisosteres for cinnamides, which are widely occurring substructures in medicinal chemistry. Starting from our lead compound 2, the introduction of additional fluoro substituents and the exchange of the methoxyphen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5356765d4b86df210beaf77646cb304
https://doi.org/10.1016/j.bmc.2014.12.012
https://doi.org/10.1016/j.bmc.2014.12.012
Autor:
Harald Hübner, Stefanie K. Fehler, Amelie L. Bartuschat, Peter Gmeiner, Sarah B. Höfling, Olaf Prante, Nuska Tschammer, Simone Maschauer, Markus R. Heinrich
Publikováno v:
Chemistry - A European Journal. 20:370-375
Introduction of [(18) F]fluoride ion into the aromatic core of phenylazocarboxylic esters was achieved in only 30 seconds, with radiochemical yields of up to 95 % (85(±10) %). For labeling purposes, the resulting (18) F-substituted azoester can be f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::048f95e095cfb10c3cc951310acce226
https://doi.org/10.1002/chem.201303409
https://doi.org/10.1002/chem.201303409
Publikováno v:
Angewandte Chemie (International ed. in English). 54(35)
Tertiary amides, which usually occur as cis/trans mixtures, can be effectively shifted to the cis conformation by placing a positive charge in close proximity to the amide carbonyl. This effect was used to prepare cis-configured prolyl amides and to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc9c273d7ebfe1a34b64fa058a3bc6ba
https://pubmed.ncbi.nlm.nih.gov/26136142
https://pubmed.ncbi.nlm.nih.gov/26136142
Autor:
Peter Gmeiner, Torsten Kuwert, Carsten Hocke, Markus R. Heinrich, Stefanie K. Fehler, Simone Maschauer, Olaf Prante, Natascha Nebel, Harald Hübner, Amelie L. Bartuschat
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(23)
A series of fluoro substituted pyridinylcarboxamides and their phenylazo analogues with high affinity and selectivity for the dopamine D3 receptor was synthesized by the use of 6-fluoropyridine-3-carbonyl chloride (1) and fluorophenylazocarboxylic es
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b207d17889b16b8eb98d59fe0d6c8813
https://pubmed.ncbi.nlm.nih.gov/25453796
https://pubmed.ncbi.nlm.nih.gov/25453796
Publikováno v:
ChemInform. 42
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::36c04a095de0c3a3a5d58360341ae837
https://doi.org/10.1002/chin.201115031
https://doi.org/10.1002/chin.201115031
Publikováno v:
Angewandte Chemie (International ed. in English). 49(50)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dda3a1a60488faf5035affc9777bd2dd
https://pubmed.ncbi.nlm.nih.gov/21064061
https://pubmed.ncbi.nlm.nih.gov/21064061