1-(Piperidin-3-yl)thymine amides as inhibitors of

Amides / chemical synthesis Antitubercular Agents / chemical synthesis Dose-Response Relationship, Drug Enzyme Inhibitors / chemical synthesis Microbial Sensitivity Tests Molecular Structure Mycobacterium tuberculosis / drug effects Nucleoside-Phosphate Kinase / antagonists & inhibitors Structure-Activity Relationship Thymine / chemical synthesis
Mycobacterium tuberculosis Thymidylate kinase inhibitors modelling

Journal

Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203

Informations de publication

Date de publication:
Dec 2019
Historique:
entrez: 12 12 2019
pubmed: 12 12 2019
medline: 18 12 2019
Statut: ppublish

Résumé

A series of readily accessible 1-(piperidin-3-yl)thymine amides was designed, synthesised and evaluated as

Identifiants

DOI: 10.1080/14756366.2019.1662790 PMID: 31822127 PMC: PMC6920704
pubmed: 31822127
doi: 10.1080/14756366.2019.1662790
pmc: PMC6920704
doi:

Substances chimiques

Amides 0
Antitubercular Agents 0
Enzyme Inhibitors 0
Nucleoside-Phosphate Kinase EC 2.7.4.4
dTMP kinase EC 2.7.4.9
Thymine QR26YLT7LT

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1730-1739

Références

ACS Infect Dis. 2016 Jun 10;2(6):393-8
pubmed: 27627627
Curr Top Med Chem. 2012;12(7):694-705
pubmed: 22283813
Eur J Med Chem. 2016 Oct 4;121:71-81
pubmed: 27236064
J Med Chem. 2015 Jan 22;58(2):753-66
pubmed: 25486447
Bioorg Med Chem. 2008 Jun 1;16(11):6075-85
pubmed: 18467107
J Biol Chem. 2003 Feb 14;278(7):4963-71
pubmed: 12454011
J Med Chem. 2004 Dec 2;47(25):6187-94
pubmed: 15566289
J Med Chem. 2003 Aug 28;46(18):3811-21
pubmed: 12930144
Eur J Med Chem. 2010 Dec;45(12):5910-8
pubmed: 20951473
J Med Chem. 2012 Nov 26;55(22):10010-21
pubmed: 23043329
J Med Chem. 2007 Nov 1;50(22):5281-92
pubmed: 17910427
J Mol Biol. 2001 Aug 3;311(1):87-100
pubmed: 11469859
Bioorg Med Chem. 2011 Dec 15;19(24):7603-11
pubmed: 22061826
J Med Chem. 2018 Apr 12;61(7):2753-2775
pubmed: 29510037
Drug Discov Today. 2017 Mar;22(3):519-525
pubmed: 27649942
Bioorg Med Chem. 2016 Nov 1;24(21):5172-5182
pubmed: 27614917
Protein Sci. 2001 Jun;10(6):1195-205
pubmed: 11369858
Bioorg Med Chem Lett. 2003 Sep 15;13(18):3045-8
pubmed: 12941330
Eur J Med Chem. 2017 Jan 27;126:491-501
pubmed: 27914363
J Comput Chem. 2009 Dec;30(16):2785-91
pubmed: 19399780
Bioorg Med Chem Lett. 2002 Oct 7;12(19):2695-8
pubmed: 12217356
ChemMedChem. 2006 Oct;1(10):1081-90
pubmed: 16921580
Chembiochem. 2002 Jan 4;3(1):108-10
pubmed: 17590962
Anal Biochem. 1994 Jul;220(1):219-21
pubmed: 7978251
ChemMedChem. 2008 Jul;3(7):1083-93
pubmed: 18418833
Curr Med Chem. 2013;20(10):1286-305
pubmed: 23394555
Chem Biodivers. 2012 Mar;9(3):536-56
pubmed: 22422522

Auteurs

Yanlin Jian (Y)

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.

Martijn D P Risseeuw (MDP)

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.

Mathy Froeyen (M)

Department of Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.

Lijun Song (L)

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.

Davie Cappoen (D)

Laboratory for Microbiology, Parasitology and Hygiene (LMPH), Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium.

Paul Cos (P)

Laboratory for Microbiology, Parasitology and Hygiene (LMPH), Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium.

Hélène Munier-Lehmann (H)

Unit of Chemistry and Biocatalysis, Department of Structural Biology and Chemistry, Institut Pasteur, CNRS UMR3523, Paris, France.

Serge van Calenbergh (S)

Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.

Articles similaires

Mathematical modeling of vancomycin release from Poly-L-Lactic Acid-Coated implants.

Papon Thamvasupong, Kwanchanok Viravaidya-Pasuwat
1.00
Vancomycin Polyesters Anti-Bacterial Agents Models, Theoretical Drug Liberation

Menthol as an effective inhibitor of quorum sensing and biofilm formation in Candida albicans and Candida glabrata by targeting the transcriptional repressor TUP1.

Pouria Khodavandi, Maryam Miri Soogh, Fahimeh Alizadeh et al.
1.00
Biofilms Candida albicans Quorum Sensing Candida glabrata Menthol

Drug repurposing against fucosyltransferase-2 via docking, STD-NMR, and molecular dynamic simulation studies.

Muhammad Atif, Humaira Zafar, Atia-Tul- Wahab et al.
1.00
Fucosyltransferases Drug Repositioning Molecular Docking Simulation Molecular Dynamics Simulation Humans

Naturally derived 3-aminoquinuclidine salts as new promising therapeutic agents.

Doris Crnčević, Alma Ramić, Andreja Radman Kastelic et al.
1.00
Humans Microbial Sensitivity Tests Anti-Bacterial Agents Biofilms Quinuclidines

Classifications MeSH

questionsmedicales.fr › Composés chimiques organiques › Amides › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Antituberculeux › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Bactéries › Bactéries à Gram positif › Bâtonnets à Gram positif › Bâtonnets asporogènes à Gram positif › Bâtonnets asporogènes réguliers à Gram positif › Mycobacteriaceae › Mycobacterium › Mycobacterium tuberculosis › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Phosphotransferases › Phosphotransferases (Phosphate Group Acceptor) › Nucleoside phosphate kinase › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › 1-(Piperidin-3-yl)thymine amides as inhibitors of
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › Pyrimidinones › Uracile › Thymine › 1-(Piperidin-3-yl)thymine amides as inhibitors of