Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors

Autor: Thomas Flagstad, Mette T. Pedersen, Tim H. Jakobsen, Jakob Felding, Tim Tolker-Nielsen, Michael Givskov, Katrine Qvortrup, Thomas E. Nielsen

Publikováno v: Flagstad, T, Pedersen, M T, Jakobsen, T H, Felding, J, Tolker-Nielsen, T, Givskov, M, Qvortrup, K & Nielsen, T E 2022, ' Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors ', Bioorganic and Medicinal Chemistry Letters, vol. 57, 128499 . https://doi.org/10.1016/j.bmcl.2021.128499
Flagstad, T, Pedersen, M T, Jakobsen, T H, Felding, J, Tolker-Nielsen, T, Givskov, M, Qvortrup, K & Nielsen, T E 2022, ' Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors ', Bioorganic & Medicinal Chemistry Letters, vol. 57, 128499 . https://doi.org/10.1016/j.bmcl.2021.128499

There is an emerging global need for new and more effective antibiotics against multi-resistant bacteria. This situation has led to massive industrial investigations on novel bacterial topoisomerase inhibitors (NBTIs) that target the vital bacterial

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04a75d8f0542497e06d1f31fa5d68338
https://curis.ku.dk/portal/da/publications/solidphase-synthesis-and-biological-evaluation-of-piperazinebased-novel-bacterial-topoisomerase-inhibitors(b50ac13f-4a93-4be7-8d32-3115e02305ca).html

Petasis/Diels-Alder/Cyclization Cascade Reactions for the Generation of Scaffolds with Multiple Stereogenic Centers and Orthogonal Handles for Library Production

Autor: Thomas Flagstad, Mads Hartvig Clausen, Carlos M. G. Azevedo, Anthony Willaume, Geanna Min, Thomas E. Nielsen, Rémy Morgentin

Publikováno v: European Journal of Organic Chemistry. 2018:5023-5029

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f9ade3a3af778e0bcd7f00c6a38f45b8
https://doi.org/10.1002/ejoc.201800565

Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions

Autor: Geanna Min, Thomas Flagstad, Mads Hartvig Clausen, Rémy Morgentin, Thomas E. Nielsen, Didier Roche, Karine Bonnet

Publikováno v: Flagstad, T, Min, G, Bonnet, K, Morgentin, R, Roche, D, Clausen, M H & Nielsen, T E 2016, ' Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions ', Organic & Biomolecular Chemistry, vol. 14, no. 21, pp. 4943-4946 . https://doi.org/10.1039/c6ob00961a

An efficient strategy for the synthesis of complex small molecules from simple building blocks is presented. Key steps of the strategy include tandem Petasis and Diels-Alder reactions, and divergent complexity-generating cyclization cascades from a k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::465394e267fbb2f4328a3f8a3fac52d0
https://orbit.dtu.dk/en/publications/5a684142-9cb9-4810-91ac-8f369607e54d

ChemInform Abstract: A Four-Component Reaction for the Synthesis of Dioxadiazaborocines

Autor: Thomas E. Nielsen, Mette Terp Petersen, Thomas Flagstad

Publikováno v: ChemInform. 46

The condensation of functionalized hydrazines (I) with boronic acids gives dioxadiazaborocines (III).

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::43ec72baa9c949e415e14d73fef876c2
https://doi.org/10.1002/chin.201546199

Combining the Petasis 3-component reaction with multiple modes of cyclization: a build/couple/pair strategy for the synthesis of densely functionalized small molecules

Autor: Thomas Flagstad, Thomas E. Nielsen, Mette Reimert Hansen, Sebastian Thordal Le Quement, Michael Givskov

Publikováno v: ACS combinatorial science. 17(1)

A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72d0ba8987114e5cfd70f1776379e366
https://pubmed.ncbi.nlm.nih.gov/25469710