Antitubercular In Vitro Drug Discovery: Tools for Begin the Search

Bueno, Juan

doi:10.5772/29634

Cited by 11 publications

(14 citation statements)

References 84 publications

(93 reference statements)

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“…The MTT measured viability of mycobacterial cells less than 70% after exposure to the MIC values for each tested compound is considered as a positive result of this assay. This low level of cell viability indicates inhibition of cell growth by inhibition of respiration [ 45 , 46 ]. It can be concluded that compounds 12 (R = 3,5-Cl, 27%), 13 (R = 3,5-CF 3 , 6%), 19 (R = 5-CF 3 -3-F, 41%), 20 (R = 5-CF 3 -2-Cl, 5%), and 21 (R = 4-CF 3 -3-F, 46%) showed the viability of M. tuberculosis that was significantly less than 70% at the tested concentration equal to MICs [ 47 ].…”

Section: Resultsmentioning

confidence: 99%

“…The percent viability is calculated through the comparison of a measured value and that of the uninhibited control: % viability = OD 570E /OD 570P × 100, where OD 570E is the reading from the compound-exposed cells, while OD 570P is the reading from the uninhibited cells (positive control). Cytotoxic potential is evaluated by percent viability <70% [ 44 , 45 , 46 , 64 ].…”

Section: Methodsmentioning

confidence: 99%

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Consensus-Based Pharmacophore Mapping for New Set of N-(disubstituted-phenyl)-3-hydroxyl-naphthalene-2-carboxamides

Bąk

Kos

Michnová

et al. 2020

IJMS

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A series of twenty-two novel N-(disubstituted-phenyl)-3-hydroxynaphthalene- 2-carboxamide derivatives was synthesized and characterized as potential antimicrobial agents. N-[3,5-bis(trifluoromethyl)phenyl]- and N-[2-chloro-5-(trifluoromethyl)phenyl]-3-hydroxy- naphthalene-2-carboxamide showed submicromolar (MICs 0.16–0.68 µM) activity against methicillin-resistant Staphylococcus aureus isolates. N-[3,5-bis(trifluoromethyl)phenyl]- and N-[4-bromo-3-(trifluoromethyl)phenyl]-3-hydroxynaphthalene-2-carboxamide revealed activity against M. tuberculosis (both MICs 10 µM) comparable with that of rifampicin. Synergistic activity was observed for the combinations of ciprofloxacin with N-[4-bromo-3-(trifluoromethyl)phenyl]- and N-(4-bromo-3-fluorophenyl)-3-hydroxynaphthalene-2-carboxamides against MRSA SA 630 isolate. The similarity-related property space assessment for the congeneric series of structurally related carboxamide derivatives was performed using the principal component analysis. Interestingly, different distribution of mono-halogenated carboxamide derivatives with the –CF3 substituent is accompanied by the increased activity profile. A symmetric matrix of Tanimoto coefficients indicated the structural dissimilarities of dichloro- and dimetoxy-substituted isomers from the remaining ones. Moreover, the quantitative sampling of similarity-related activity landscape provided a subtle picture of favorable and disallowed structural modifications that are valid for determining activity cliffs. Finally, the advanced method of neural network quantitative SAR was engaged to illustrate the key 3D steric/electronic/lipophilic features of the ligand-site composition by the systematic probing of the functional group.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Consensus-Based Pharmacophore Mapping for New Set of N-(disubstituted-phenyl)-3-hydroxyl-naphthalene-2-carboxamides

Bąk

Kos

Michnová

et al. 2020

IJMS

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“…For the purpose of this assay, a measured viability of M. tuberculosis H37Ra of less than 70%, as determined by MTT, after exposure to the MIC of each test compound (as determined by the alamarBlue assay) was considered a positive result. As such, a low level of cell viability may suggest inhibition of cell growth through respiratory inhibition 48. Model compounds selected from 14 derivatives with the highest antitubercular derivatives, showed less than 70% viability of M. tuberculosis H37Ra at the lowest tested concentration (8 µg/mL, i.e.…”

mentioning

confidence: 99%

Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents

Kos

Zadražilová

Nevin

et al. 2015

Bioorganic & Medicinal Chemistry

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“…The MTT assay is a well-characterized method of assessing cell growth through measurement of respiration. As such, a low level of cell viability may suggest inhibition of cell growth through respiratory inhibition [49]. 3-Methoxy ( 2b ) and 4-methyl ( 3c ) derivatives showed more than 80% reduction in activity at the lowest tested concentration (8 µg/mL, i.e.…”

Section: Resultsmentioning

confidence: 99%

Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides

et al. 2014

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Abstract:In this study, a series of twenty-two ring-substituted naphthalene-1-carboxanilides were prepared and characterized. Primary in vitro screening of the synthesized carboxanilides was performed against Mycobacterium avium subsp.and N-(3-fluorophenyl)naphthalene-1-carboxamide showed against M. avium subsp. paratuberculosis two-fold higher activity than rifampicin and three-fold higher activity than ciprofloxacin. The most effective antimycobacterial compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. The testing of biological activity of the compounds was completed with the study of photosynthetic electron transport (PET) inhibition in isolated spinach (Spinacia oleracea L.) chloroplasts. The PET-inhibiting activity expressed -[4-(trifluoromethyl)phenyl]naphthalene-1-carboxamide was 59 μmol/L. The structure-activity relationships are discussed.

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Antitubercular In Vitro Drug Discovery: Tools for Begin the Search

Cited by 11 publications

References 84 publications

Consensus-Based Pharmacophore Mapping for New Set of N-(disubstituted-phenyl)-3-hydroxyl-naphthalene-2-carboxamides

Consensus-Based Pharmacophore Mapping for New Set of N-(disubstituted-phenyl)-3-hydroxyl-naphthalene-2-carboxamides

Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents

Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides

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