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3 results on '"mammalian cellular viability"'

1. Synthesis and Antimycobacterial Activity of 3-Phenyl-1H-indoles

Author

Renata Jardim Etchart, Raoní S. Rambo, Bruno Lopes Abbadi, Nathalia Sperotto, Christiano Ev Neves, Fernanda Fries Silva, Maiele Dornelles, Lovaine Duarte, Fernanda Souza Macchi, Marcia Alberton Perelló, Rogério Vescia Lourega, Cristiano Valim Bizarro, Luiz Augusto Basso, and Pablo Machado

Subjects
1H-indoles, Mycobacterium tuberculosis, mammalian cellular viability, genotoxicity, time-kill, pharmacodynamic model, Organic chemistry, QD241-441
Abstract

Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20 1H-indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Furthermore, the top hit compounds were active against multidrug-resistant strains, without cross-resistance with first-line drugs. Exposing HepG2 and Vero cells to the molecules for 72 h showed that one of the evaluated structures was devoid of apparent toxicity. In addition, this 3-phenyl-1H-indole showed no genotoxicity signals. Finally, time-kill and pharmacodynamic model analyses demonstrated that this compound has bactericidal activity at concentrations close to the Minimum Inhibitory Concentration, coupled with a strong time-dependent behavior. To the best of our knowledge, this study describes the activity of 3-phenyl-1H-indole against Mtb for the first time.

Published
2021
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2. Synthesis and Antimycobacterial Activity of 3-Phenyl-1H-indoles

Author

Christiano Ev Neves, Renata Jardim Etchart, Bruno Lopes Abbadi, Luiz Augusto Basso, Raoní S. Rambo, Marcia Alberton Perelló, Cristiano Valim Bizarro, Fernanda Souza Macchi, Maiele Dornelles, Fernanda Fries Silva, Rogério Vescia Lourega, Lovaine Duarte, Pablo Machado, and Nathalia D. M. Sperotto

Subjects
Tuberculosis, Indoles, medicine.drug_class, Antitubercular Agents, Pharmaceutical Science, Organic chemistry, Microbial Sensitivity Tests, medicine.disease_cause, Antimycobacterial, Article, Analytical Chemistry, Microbiology, Mycobacterium tuberculosis, Minimum inhibitory concentration, mammalian cellular viability, Structure-Activity Relationship, QD241-441, Cell Line, Tumor, Drug Discovery, Chlorocebus aethiops, medicine, Animals, Humans, Physical and Theoretical Chemistry, Vero Cells, pharmacodynamic model, biology, Chemistry, genotoxicity, Hep G2 Cells, 1H-indoles, time-kill, medicine.disease, biology.organism_classification, In vitro, Chemistry (miscellaneous), Toxicity, Vero cell, Molecular Medicine, Genotoxicity
Abstract

Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20 1H-indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Furthermore, the top hit compounds were active against multidrug-resistant strains, without cross-resistance with first-line drugs. Exposing HepG2 and Vero cells to the molecules for 72 h showed that one of the evaluated structures was devoid of apparent toxicity. In addition, this 3-phenyl-1H-indole showed no genotoxicity signals. Finally, time-kill and pharmacodynamic model analyses demonstrated that this compound has bactericidal activity at concentrations close to the Minimum Inhibitory Concentration, coupled with a strong time-dependent behavior. To the best of our knowledge, this study describes the activity of 3-phenyl-1H-indole against Mtb for the first time.

Published
2021

3. Synthesis and Antimycobacterial Activity of 3-Phenyl-1 H -indoles.

Author

Jardim Etchart, Renata, Rambo, Raoní S., Lopes Abbadi, Bruno, Sperotto, Nathalia, Ev Neves, Christiano, Fries Silva, Fernanda, Dornelles, Maiele, Duarte, Lovaine, Souza Macchi, Fernanda, Alberton Perelló, Marcia, Vescia Lourega, Rogério, Valim Bizarro, Cristiano, Basso, Luiz Augusto, and Machado, Pablo

Subjects
*MYCOBACTERIUM tuberculosis, *GENETIC toxicology, *TUBERCULOSIS, *WORLD health
Abstract

Tuberculosis has been described as a global health crisis since the 1990s, with an estimated 1.4 million deaths in the last year. Herein, a series of 20 1H-indoles were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Furthermore, the top hit compounds were active against multidrug-resistant strains, without cross-resistance with first-line drugs. Exposing HepG2 and Vero cells to the molecules for 72 h showed that one of the evaluated structures was devoid of apparent toxicity. In addition, this 3-phenyl-1H-indole showed no genotoxicity signals. Finally, time-kill and pharmacodynamic model analyses demonstrated that this compound has bactericidal activity at concentrations close to the Minimum Inhibitory Concentration, coupled with a strong time-dependent behavior. To the best of our knowledge, this study describes the activity of 3-phenyl-1H-indole against Mtb for the first time. [ABSTRACT FROM AUTHOR]

Published
2021
Full Text
View/download PDF

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