scholarly journals In vitro evaluation of the inhibitory effect of 3, 5-dichloro-2- pyridone on Mycobacterium tuberculosis H37Rv

2020 ◽  
Vol 19 (1) ◽  
pp. 163-168
Author(s):  
Lin Ling ◽  
Chen Ling ◽  
Hua Wu
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Bovine Serum ◽  
Antimicrobial Effect ◽  
Bactericidal Effect ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Current Treatment ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv

Purpose: To investigate the anti-tuberculosis potential of twelve commercially available pyridone analogues against Mycobacterium tuberculosis H37Rv strain.Methods: Twelve commercially available pyridone-based compounds were screened against M. tuberculosis H37Rv using different susceptibility tests. The most active or lead compound was further evaluated in detail for its anti-tuberculosis (anti-TB) potential. Kill kinetics was used to determine the dynamics of its anti-TB activity in vitro.Results: Compounds d, j and k were potent against M. tuberculosis H37Rv, with minimum inhibitory concentrations (MICs) of 10, 5 and 10 μg/mL, respectively. The standard anti-TB drugs used in this study (positive control drugs) demonstrated MIC of 2.5 μg/mL. The anti-TB effect of compound j was comparable with those of the standard drugs (RIF, LVX, AMK, EMB and INH). The minimum bactericidal concentration (MBC) of compound j was 10 μg/mL. It produced an MIC of 5 μg/mL in agar proportion method (APM). However, its MIC in Middlebrook 7H9 broth supplemented with 10 % fetal bovine serum (FBS) and 4 % bovine serum albumin (BSA) increased 4- and 8-fold, respectively. The bactericidal effect of compound j was time- and concentration-dependent at dilutions above 2x MIC. Combination of compound j with RIF, LVX or AMK exhibited fractional inhibitory concentration index (ΣFIC) of 1, indicative of additive drug-drug interactions. However, combination with INH or EMB produced a ΣFIC of 2. None of the tested drug combinations was antagonistic.Conclusion: Compound j exhibits potent time- and concentration-dependent antimicrobial effect against M. tuberculosis H37Rv. Thus, it may be suitable as an adjunct to current treatment of drug sensitive and drug-resistant TB. Keywords: Tuberculosis, Mycobacterium tuberculosis, Pyridone analogs, Antimicrobial activity, Antibiotics

In vitro Anti Mycobacterium tuberculosis H37Rv Activity of Lannea acida A. Rich from Burkina Faso

2010 ◽  
Vol 14 (1) ◽  
pp. 47-52 ◽  
Author(s):  
L. Ouattara ◽  
J. Koudou ◽  
D.S. Karou ◽  
L. Giaco ◽  
G. Capelli ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Burkina Faso ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv

Effect of exogenous cardiolipin on the growth and viability of Mycobacterium tuberculosis H37Rv in vitro

2010 ◽  
Vol 434 (1) ◽  
pp. 371-374 ◽  
Author(s):  
S. N. Andreevskaya ◽  
T. G. Smirnova ◽  
Yu. A. Zhogina ◽  
D. I. Smirnova ◽  
Yu. L. Mikulovich ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv

scholarly journals Isoniazid-Isatin Hydrazone Derivatives: Synthesis, Antitubercular Activity and Molecular Docking Studies

2021 ◽  
Vol 18 (21) ◽  
pp. 39
Author(s):  
Mardi Santoso ◽  
Muhammad Riza Ghulam Fahmi ◽  
Yehezkiel Steven Kurniawan ◽  
Taslim Ersam ◽  
Sri Fatmawati ◽  
...  
Keyword(s):  
Hydrogen Bonding ◽  
Mycobacterium Tuberculosis ◽  
Molecular Docking ◽  
Active Site ◽  
Antitubercular Activity ◽  
Docking Study ◽  
Positive Control ◽  
Tuberculosis H37rv ◽  
Molecular Docking Study

This study examined the synthesis of isoniazid-isatin hydrazone derivatives 5-7, followed by an investigation on the in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv, and molecular docking. A yield of 81 - 92 % of these compounds was achieved, with structural characterization by spectroscopic methods (FTIR, NMR, HRMS). The in vitro antitubercular activity was evaluated against M. tuberculosis H37Rv, and the highest effect was observed in compound 7, with a minimum inhibitory concentration (MIC) of 0.017 mM, lower than rifampicin (MIC 0.048 mM), which served as the positive control. In addition, the molecular docking of 5-7 was performed to visualize the interaction of isoniazid-isatin hydrazone derivatives with the active site of InhA receptor, which was in agreement with the experimental data. The hydrogen bonding with Ser94 and pi-pi interaction with Phe41 and/or Phe97 on the InhA active site was pivotal for the antitubercular activity. HIGHLIGHTS Tuberculosis caused by Mycobacterium tuberculosis is one of the top ten leading causes of death globally The first and second lines of antituberculosis drugs are the prevalent treatment for this disease, but they show several drawbacks and are exacerbated by the occurrence of drug resistance The isoniazid-isatin hydrazone derivatives were designed through molecular hybridization and synthesized effectively and exhibited moderate to high activity against tuberculosis H37Rv Molecular docking study demonstrated that the hydrogen bonding with Ser94 and the pi-pi interaction with Phe41 and/or Phe97 are important for antitubercular activity GRAPHICAL ABSTRACT

scholarly journals BIOAKTIVITAS DAN STUDI IN SILICO SENYAWA TURUNAN N’-BENZOYLISONICOTINOHYDRAZIDE (4-methyl, 4-chloro dan 3,5-dinitro) PADA Mycobacterium Tuberculosis (H37RV) BAKTERI GRAM POSITIF SERTA BAKTERI GRAM NEGATIF

2019 ◽  
Vol 2 (1) ◽  
pp. 37-48
Author(s):  
Ruswanto Ruswanto
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Binding Affinity ◽  
In Silico ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv ◽  
Microtiter Assay

Isoniazid merupakan obat antituberkulosis yang memiliki aktivitas antimikobakterial yang baik yang bekerja secara aktif dengan menghambat biosintesis asam mikolat. Telah dilakukan pengujian In Vitro pada senyawa N’-(4-Methylbenzoyl) Isonicotinohydrazide N’-(4-Chlorobenzoyl) Isonicotinohydrazide dan N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide terhadap Mycobacterium tuberculosis H37Rv, bakteri gram positif serta bakteri gram negatif dengan menggunakan metode sumuran dan pada pengujian Mycobacterium tuberculosis H37Rv menggunakan metode REMA (Resazurin Microtiter Assay). Didapat nilai MIC terbaik pada senyawa N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide memiliki potensi tinggi sebagai antibakteri dengan nilai MIC 0,169 ppm terhadap bakteri e.colli. Ketiga senyawa yang diujikan pada  Mycobacterium tuberculosis H37Rv memiliki kemampuan sebagai anti tuberkulosis tetapi isoniazid lebih baik dari senyawa uji. Senyawa N’-(3,5-Dinitrobenzoyl) Isonicotinohydrazide di dockingkan pada reseptor 1KZN memiliki binding affinity yang lebih kecil dibandingkan senyawa pembanding yaitu isoniazid sebesar -6,89 kkal/mol.

scholarly journals Synthesis of Tetrahydro-2H-[1,3,5]thiadiazine-5-(4-pyridylcarboxamido)-2-thione with antitubercular activity

2004 ◽  
Vol 72 (1) ◽  
pp. 35-41 ◽  
Author(s):  
D. Sriram ◽  
K. Jyothi Mallika ◽  
P. Yogeeswari
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
Therapeutic Use ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv ◽  
Radiometric System ◽  
Elemental Analyses ◽  
Derivatives Of

3-Substituted-5-(4-pyridylcarboxamide)tetrahydro-2H-[1,3,5]thiadizine-2-thione derivatives (1-9) were synthesized as derivatives of isoniazid (INH) to overcome the resistance developed with its therapeutic use. The structures were confirmed by their spectral and elemental analyses data. These derivatives revealed higher lipophilicity compared with INH. The antimycobacterial activity of the synthesized compounds and INH was evaluated in vitro against Mycobacterium tuberculosis H37Rv at 6.25 µg/ml in BACTEC 12B medium using the BACTEC 460 radiometric system. The derivatives exhibited antitubercular activity.

scholarly journals In Vitro Antimicrobial Effect of a Cold Plasma Jet against Enterococcus faecalis Biofilms

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Chunqi Jiang ◽  
Christoph Schaudinn ◽  
David E. Jaramillo ◽  
Paul Webster ◽  
J. William Costerton
Keyword(s):  
Enterococcus Faecalis ◽  
Cold Plasma ◽  
Plasma Jet ◽  
Antimicrobial Effect ◽  
Bactericidal Effect ◽  
Positive Control ◽  
Negative Control ◽  
Reactive Plasma ◽  
Bacterial Cell Morphology

The hypothesis that a cold plasma jet has the antimicrobial effect against Enterococcus faecalis biofilms was tested in vitro. 27 hydroxyapatite discs were incubated with E. faecalis for six days to form a monoculture biofilm on the disc surface. The prepared substrata were divided into three groups: the negative control, the positive control (5.25% NaOCl solution), and the plasma treatment group. Resultant colony-forming unit counts were associated with observations of bacterial cell morphology changes using scanning electron microscopy (SEM). Treatment of E. faecalis biofilm with the plasma and 5.25% NaOCl for 5 min resulted in 93.1% and 90.0% kill (P<0.0001), respectively. SEM detected that nearly no intact bacteria were discernible for the plasma-exposed HA disc surfaces. The demonstrated bactericidal effect of the plasma with direct surface contact may be due to the enhanced oxidation by the locally produced reactive plasma species.

scholarly journals In Vitro Interactions of Costus speciosus (J. Koenig) Sm., Cymbopogon citratus (Dc. Ex Nees) Stapf. and Tabernaemontana coronaria (L.) Willd. with First-Line Anti-Tuberculosis Drugs Against Mycobacterium tuberculosis H37rv

2021 ◽  
Vol 19 (2) ◽  
pp. 171-178
Author(s):  
Suriyati Mohamad ◽  
◽  
Nur Najihah Ismail ◽  
Hasnah Osman ◽  
Habibah A Wahab ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Tuberculosis H37rv ◽  
Cymbopogon Citratus ◽  
First Line ◽  
Additive Interaction ◽  
Mycobacterium Tuberculosis H37rv ◽  
Costus Speciosus ◽  
Drug Leads ◽  
Leaf N

Global tuberculosis (TB) burden underscores the importance of developing new effective anti-TB drugs. This study was concerned with prospecting for potential anti-TB agents from Malaysian medicinal plants. In our previous study, we have reported that n-hexane fractions of Costus speciosus (C. speciosus) (J. Koening) Sm., Cymbopogon citratus (C. citratus ) (DC.) Stapf. and Tabernaemontana coronaria (T. coronaria) (Jacq.) posses promising anti-TB activity against Mycobacterium tuberculosis (M. tuberculosis) H37Rv with minimum inhibitory concentrations (MICs) of 200–100 µg/mL. This study aimed to investigate the interactions of these active fractions with first-line anti-TB drugs (isoniazid, rifampicin, ethambutol and streptomycin) against M. tuberculosis H37Rv using the microdilution checkerboard method. C. citratus (stem-rhizome) n-hexane fraction exhibited synergism with all drugs except ethambutol which showed additive interaction. Synergistic was also observed when C. speciosus (stem-flower) n-hexane and T. coronaria (leaf) n-hexane fractions in combination with rifampicin. C. speciosus (stem-flower) n-hexane and T. coronaria (leaf) n-hexane exhibited additive interaction with isoniazid, ethambutol and streptomycin. Hence, these active plants are worthy of further investigations for the discovery of anti-TB drug leads.

SYNTHESIS OF SOME NOVEL 1,2,4-TRIAZOLE ANALOGUES AS POTENTIAL ANTI-TUBERCULAR AGENTS

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 41-47
Author(s):  
R. R Somani ◽  
◽  
G. K Shinde ◽  
P.Y. Shirodkar ◽  
G. J. Sanap
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Tuberculosis H37rv ◽  
Triazole Derivatives ◽  
Mycobacterium Tuberculosis H37rv ◽  
Elemental Analyses

A series of 5-(N-substituted carboxamidoethylthio)-3-(3’pyridyl)-4-amino-1,2,4-triazole derivatives (6a-j) were synthesized and evaluated for anti-tubercular activity. The derivatives were purified and structures were elucidated by spectral and elemental analyses. They were screened in-vitro at 10µg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). Compounds 6e and 6h were found active as they exhibited IC50 and IC90 values at < 100µg/mL.

Sign in / Sign up

Export Citation Format

Share Document