New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents.


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: 21 3 2019
pubmed: 21 3 2019
medline: 6 4 2019
Statut: ppublish

Résumé

Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro moiety, leading to the disclosure of a new lead exhibiting a strong activity against MbtI. Our best candidate 1 h displayed a K

Identifiants

pubmed: 30889995
doi: 10.1080/14756366.2019.1589462
pmc: PMC6427685
doi:

Substances chimiques

Antitubercular Agents 0
Enzyme Inhibitors 0
Furans 0
Lyases EC 4.-
salicylate synthetase EC 4.-

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

823-828

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Auteurs

Laurent R Chiarelli (LR)

a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.

Matteo Mori (M)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

Giangiacomo Beretta (G)

c Department of Environmental Science and Policy , University of Milano , Milano , Italy.

Arianna Gelain (A)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

Elena Pini (E)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

Josè Camilla Sammartino (JC)

a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.

Giovanni Stelitano (G)

a Department of Biology and Biotechnology "L Spallanzani" , University of Pavia , Pavia , Italy.

Daniela Barlocco (D)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

Luca Costantino (L)

d Department of Life Sciences , University of Modena e Reggio Emilia , Modena , Italy.

Margherita Lapillo (M)

e Department of Pharmacy , University of Pisa , Pisa , Italy.

Giulio Poli (G)

e Department of Pharmacy , University of Pisa , Pisa , Italy.

Isabella Caligiuri (I)

f Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.

Flavio Rizzolio (F)

f Pathology Unit, Department of Molecular Biology and Translational Research , National Cancer Institute and Center for Molecular Biomedicine , Aviano , Italy.
g Department of Molecular Science and Nanosystems , Ca' Foscari University of Venezia , Venezia-Mestre , Italy.

Marco Bellinzoni (M)

h Institut Pasteur , Paris , France.

Tiziano Tuccinardi (T)

e Department of Pharmacy , University of Pisa , Pisa , Italy.

Stefania Villa (S)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

Fiorella Meneghetti (F)

b Department of Pharmaceutical Sciences , University of Milano , Milano , Italy.

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Classifications MeSH