Ligand Growing Experiments Suggested 4-amino and 4-ureido pyridazin-3(2

FABP4 FABP4 inhibitors FABP4is computing assisted molecular design fatty acid binding protein pyridazinone

Journal

Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453

Informations de publication

Date de publication:
28 Oct 2022
Historique:
received: 06 10 2022
revised: 21 10 2022
accepted: 21 10 2022
entrez: 10 11 2022
pubmed: 11 11 2022
medline: 11 11 2022
Statut: epublish

Résumé

Fatty acid binding protein (FABP4) inhibitors are of synthetic and therapeutic interest and ongoing clinical studies indicate that they may be a promise for the treatment of cancer, as well as other diseases. As part of a broader research effort to develop more effective FABP4 inhibitors, we sought to identify new structures through a two-step computing assisted molecular design based on the established scaffold of a co-crystallized ligand. Novel and potent FABP4 inhibitors have been developed using this approach and herein we report the synthesis, biological evaluation and molecular docking of the 4-amino and 4-ureido pyridazinone-based series.

Identifiants

pubmed: 36355506
pii: ph15111335
doi: 10.3390/ph15111335
pmc: PMC9697826
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Coordination for the Improvement of Higher Education Personnel - Brazil
ID : CAPES-PRINT, funding number 88887.570120/2020-00

Références

J Mol Graph Model. 2000 Jun;18(3):273-82
pubmed: 11021543
Bioorg Med Chem. 2010 Nov 15;18(22):7890-9
pubmed: 20937560
PLoS One. 2013 Nov 14;8(11):e79386
pubmed: 24244493
Eur J Med Chem. 2018 Jan 1;143:583-590
pubmed: 29207341
J Med Chem. 1989 Mar;32(3):528-37
pubmed: 2563772
ChemMedChem. 2018 Jul 6;13(13):1336-1342
pubmed: 29693778
Drug Test Anal. 2021 Nov;13(11-12):1871-1887
pubmed: 34665524
J Med Chem. 2009 Aug 27;52(16):5044-57
pubmed: 19639995
Eur J Med Chem. 2022 Oct 5;240:114604
pubmed: 35849941
Int J Mol Sci. 2019 Feb 21;20(4):
pubmed: 30795625
Nat Rev Drug Discov. 2008 Jun;7(6):489-503
pubmed: 18511927
Biochim Biophys Acta. 2006 Feb;1761(2):172-81
pubmed: 16574478
J Chem Inf Model. 2014 Nov 24;54(11):3046-50
pubmed: 25360897
Nat Rev Endocrinol. 2015 Oct;11(10):592-605
pubmed: 26260145
Bioorg Chem. 2019 Mar;84:276-284
pubmed: 30529845
Curr Pharm Biotechnol. 2006 Dec;7(6):467-82
pubmed: 17168664
BMC Cancer. 2011 Jul 18;11:302
pubmed: 21767383
Bioorg Med Chem. 2010 May 15;18(10):3506-17
pubmed: 20413313
Int J Clin Pract Suppl. 2004 Oct;(143):9-21
pubmed: 16035392
Nat Med. 2011 Oct 30;17(11):1498-503
pubmed: 22037646
Bioorg Med Chem. 2016 Apr 8;:
pubmed: 27134116
Data Brief. 2018 Dec 19;22:471-483
pubmed: 30619925
Bioorg Chem. 2021 Dec;117:105428
pubmed: 34710668
PLoS One. 2012;7(11):e48605
pubmed: 23139800
J Biol Chem. 2009 May 15;284(20):13473-13480
pubmed: 19318353
Mar Drugs. 2019 Oct 31;17(11):
pubmed: 31683588
Biochim Biophys Acta. 2000 Jun 26;1486(1):28-44
pubmed: 10856711
Atherosclerosis. 2006 Sep;188(1):102-11
pubmed: 16313911
Cancer Cell Int. 2020 Oct 19;20:512
pubmed: 33088219
J Mol Model. 2004 Apr;10(2):155-64
pubmed: 14997367
Endocrinol Metab Clin North Am. 2008 Sep;37(3):635-46, viii-ix
pubmed: 18775356
Nat Commun. 2018 Jul 26;9(1):2923
pubmed: 30050129
Int J Cancer. 2014 Dec 1;135(11):2558-68
pubmed: 24740818
Placenta. 2016 Oct;46:49-62
pubmed: 27697222
Ann Intern Med. 1997 Jan 15;126(2):137-45
pubmed: 9005748
Eur Rev Med Pharmacol Sci. 2018 Nov;22(22):7807-7818
pubmed: 30536325
J Med Chem. 2009 Dec 10;52(23):7397-409
pubmed: 19788200
Bioorg Med Chem. 2016 Sep 15;24(18):4310-4317
pubmed: 27460668
J Comput Aided Mol Des. 1990 Mar;4(1):1-105
pubmed: 2197373
Bioorg Chem. 2018 Dec;81:334-339
pubmed: 30189413
Front Biosci. 1998 Feb 15;3:d169-75
pubmed: 9450985
J Chem Inf Model. 2006 Mar-Apr;46(2):665-76
pubmed: 16562997
Bioorg Med Chem. 2007 Aug 15;15(16):5563-75
pubmed: 17548197
Eur J Med Chem. 2015 Jan 7;89:32-41
pubmed: 25462223
Eur J Med Chem. 2017 Sep 29;138:854-873
pubmed: 28738306
J Enzyme Inhib Med Chem. 2020 Dec;35(1):1137-1144
pubmed: 32367744

Auteurs

Letizia Crocetti (L)

Dipartimento NEUROFARBA-Pharmaceutical and Nutraceutical Section, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.

Giuseppe Floresta (G)

Dipartimento di Scienze del Farmaco e della Salute, Università di Catania, Viale A. Doria 6, 95125 Catania, Italy.

Chiara Zagni (C)

Dipartimento di Scienze del Farmaco e della Salute, Università di Catania, Viale A. Doria 6, 95125 Catania, Italy.

Divya Merugu (D)

Institute of Pharmaceutical Science, King's College London, Stamford Street, London SE1 9NH, UK.

Francesca Mazzacuva (F)

School of Health, Sport and Bioscience, University of East London, London E15 4LZ, UK.

Renan Rodrigues de Oliveira Silva (RR)

Institute of Pharmaceutical Science, King's College London, Stamford Street, London SE1 9NH, UK.

Claudia Vergelli (C)

Dipartimento NEUROFARBA-Pharmaceutical and Nutraceutical Section, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.

Maria Paola Giovannoni (MP)

Dipartimento NEUROFARBA-Pharmaceutical and Nutraceutical Section, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.

Agostino Cilibrizzi (A)

Institute of Pharmaceutical Science, King's College London, Stamford Street, London SE1 9NH, UK.
Medicines Development, Centre for Therapeutic Innovation, University of Bath, Bath BA2 7AY, UK.

Classifications MeSH