(Heteroarylmethyl)benzoic Acids as a New Class of Bacterial Cystathionine γ-Lyase Inhibitors: Synthesis, Biological Evaluation, and Molecular Modeling.

MRSA antibiotic potentiator antimicrobial resistance bCSE biologically active molecules indole derivatives sepsis

Journal

ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580

Informations de publication

Date de publication:
21 May 2024
Historique:
medline: 21 5 2024
pubmed: 21 5 2024
entrez: 21 5 2024
Statut: aheadofprint

Résumé

Antibiotic resistance is one of the most serious global health threats. Therefore, there is a need to develop antimicrobial agents with new mechanisms of action. Targeting of bacterial cystathionine γ-lyase (bCSE), an enzyme essential for bacterial survival, is a promising approach to overcome antibiotic resistance. Here, we described a series of (heteroarylmethyl)benzoic acid derivatives and evaluated their ability to inhibit bCSE or its human ortholog hCSE using known bCSE inhibitor NL2 as a lead compound. Derivatives bearing the 6-bromoindole group proved to be the most active, with IC

Identifiants

pubmed: 38771206
doi: 10.1021/acsinfecdis.4c00136
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Auteurs

Anastasia Golovina (A)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Eleonora Proia (E)

Rome Center for Molecular Design, Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5 , Rome 00185, Italy.

Francesco Fiorentino (F)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, Rome 00185, Italy.

Maxim Yunin (M)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Maria Kasatkina (M)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Nailya Zigangirova (N)

National Research Centre of Epidemiology and Microbiology named after N. F. Gamaleya, Russian Health Ministry, Gamaleya St.18 , 123098 Moscow, Russia.

Anna Soloveva (A)

National Research Centre of Epidemiology and Microbiology named after N. F. Gamaleya, Russian Health Ministry, Gamaleya St.18 , 123098 Moscow, Russia.

Elena Sysolyatina (E)

National Research Centre of Epidemiology and Microbiology named after N. F. Gamaleya, Russian Health Ministry, Gamaleya St.18 , 123098 Moscow, Russia.

Svetlana Ermolaeva (S)

National Research Centre of Epidemiology and Microbiology named after N. F. Gamaleya, Russian Health Ministry, Gamaleya St.18 , 123098 Moscow, Russia.

Roman Novikov (R)

Engelhardt Institute of Molecular Biology of the Russian Academy of Sciences, 32 Vavilov St. , Moscow 119991, Russia.

Sergei Silonov (S)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.
Laboratory of Structural Dynamics, Stability and Folding of Proteins, Institute of Cytology, Russian Academy of Sciences, 4 Tikhoretsky Avenue , St. Petersburg 194064, Russia.

Sergei Pushkin (S)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Milan Mladenović (M)

Kragujevac Center for Computational Biochemistry, Department of Chemistry, Faculty of Science, University of Kragujevac, Radoja Domanovića 12 , Kragujevac 34000, P.O. Box 60, Serbia.

Julia Isakova (J)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Albina Belik (A)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Maxim Nawrozkij (M)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Dante Rotili (D)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5, Rome 00185, Italy.

Rino Ragno (R)

Rome Center for Molecular Design, Department of Drug Chemistry and Technologies, Sapienza University of Rome, P. le A. Moro 5 , Rome 00185, Italy.

Roman Ivanov (R)

Sirius University of Science and Technology, Olympic Avenue, 1, Sirius , Krasnodar Region 354340, Russia.

Classifications MeSH