SAR Studies of the Leupyrrins: Design and Total Synthesis of Highly Potent Simplified Leupylogs.

Leupylogs SAR studies antifungal agents natural products total synthesis

Journal

Chemistry (Weinheim an der Bergstrasse, Germany)
ISSN: 1521-3765
Titre abrégé: Chemistry
Pays: Germany
ID NLM: 9513783

Informations de publication

Date de publication:
26 Nov 2020
Historique:
received: 29 05 2020
pubmed: 2 7 2020
medline: 2 7 2020
entrez: 2 7 2020
Statut: ppublish

Résumé

Leupyrrins are highly potent antifungal agents. A structure-activity-relationship study of natural and synthetic derivatives is reported which reveals important insights into the biological relevance of several structural subunits leading to the discovery of highly potent but drastically simplified leupylogs that incorporate a stable and readily available aromatic side chain. For their synthesis a concise strategy is described that enables a short and versatile access.

Identifiants

pubmed: 32608026
doi: 10.1002/chem.202002622
pmc: PMC7756798
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

15074-15078

Subventions

Organisme : Deutsche Forschungsgemeinschaft
ID : TRR 261
Organisme : Deutsche Forschungsgemeinschaft
ID : ME 2756/7-1
Organisme : Deutsche Forschungsgemeinschaft
ID : GK 850

Informations de copyright

© 2020 The Authors. Published by Wiley-VCH GmbH.

Références

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5807-10
pubmed: 19713106
J Nat Prod. 2003 Sep;66(9):1203-6
pubmed: 14510597
J Med Chem. 2015 Jun 11;58(11):4839-44
pubmed: 25990761
Microb Cell Fact. 2013 Sep 24;12:85
pubmed: 24063434
J Med Chem. 2020 Feb 27;63(4):1684-1698
pubmed: 31990540
Chemistry. 2017 Mar 8;23(14):3300-3320
pubmed: 27906488
Org Lett. 2016 Aug 19;18(16):3964-7
pubmed: 27486674
Org Biomol Chem. 2015 May 21;13(19):5302-43
pubmed: 25829247
J Am Chem Soc. 2015 Apr 1;137(12):4086-9
pubmed: 25769018
Chemistry. 2020 Nov 26;26(66):15074-15078
pubmed: 32608026
Eur J Med Chem. 2005 Feb;40(2):143-54
pubmed: 15694649
J Org Chem. 2004 Sep 3;69(18):6131-3
pubmed: 15373501
J Org Chem. 2010 May 21;75(10):3507-10
pubmed: 20373742
J Org Chem. 2004 Mar 19;69(6):1822-30
pubmed: 15058924

Auteurs

Paul R Wosniok (PR)

Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121, Bonn, Germany.
Current address: Eurofins Umwelt West GmbH Wesseling, Vorgebirgsstrasse 20, 50389 Wesseling, Germany.

Christopher Knopf (C)

Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121, Bonn, Germany.
Current address: Eurofins Umwelt West GmbH Wesseling, Eurofins Genomics Europe Synthesis GmbH, Anzinger Str. 7a, 85560 Ebersberg, Germany.

Sandra Dreisigacker (S)

Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121, Bonn, Germany.
Current address: HWI pharma services GmbH, Rheinzaberner Straße 8, 76761, Ruelzheim, Germany.

J Manuel Orozco-Rodriguez (JM)

Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124, Braunschweig, Germany.

Bettina Hinkelmann (B)

Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124, Braunschweig, Germany.

Peter P Mueller (PP)

Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124, Braunschweig, Germany.

Mark Brönstrup (M)

Helmholtz Centre for Infection Research, Inhoffenstraße 7, 38124, Braunschweig, Germany.

Dirk Menche (D)

Kekulé-Institut für Organische Chemie und Biochemie, Universität Bonn, Gerhard-Domagk-Str. 1, 53121, Bonn, Germany.

Classifications MeSH