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 Novel Pyrimidine Derivatives from 2,5-Dichloro-3-acetylthienyl Chalcones as Antifungal, Antitubercular and Cytotoxic Agents: Design, Synthesis, Biological Activity and Docking Study

2019 ◽  
Vol 31 (6) ◽  
pp. 1212-1220
Author(s):  
BONTHA VENKATA SUBRAHMANYA LOKESH ◽  
Y. RAJENDRA PRASAD ◽  
AFZAL BASHA SHAIK
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Binding Affinity ◽  
Crystalline Structure ◽  
Candida Tropicalis ◽  
Fungal Species ◽  
Tuberculosis H37rv ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Mycobacterium Tuberculosis H37rv

Twenty novel pyrimidine derivatives were synthesized from 2,5-dichloro-3-acetylthienyl chalcones by reacting with guanidine HCl in presence of KOH and ethanol under reflux for 6 h. Their structural characterizations were evaluated by ATR-FTIR, 1H NMR, 13C NMR, mass spectroscopy. They were also screened for antifungal, antitubercular and cytotoxicity activities. They were displayed good antifungal activity (MIC = 32-125 μg/mL) against Aspergillus niger and Candida tropicalis fungal species except compound 15 with 4"-pyridinyl moiety (MIC = 8.00 μg/mL) being more potent. Compound 5 with 2",4"-dichlorophenyl moiety was shown with good antitubercular activity (MIC = 6.2 μg/mL) against Mycobacterium tuberculosis H37Rv (MTB) stain. They have also tested for in vitro cytotoxicity activity against DU-145 prostate cancer cell lines. In which the compound 15 with 4"-pyridinyl moiety (IC50 = 2.0 ± 0.1 μg/mL) and compound 17 with 2"-pyrrolyl moiety (IC50 = 6.0 ± 0.1 μg/mL) possess highly potent antiprostate cancer properties. The molecular docking was done with the crystalline structure of mitochondrial 2-enoyl thioester reductase Etr1p/Etr2p heterodimer from Candida tropicalis fungal species with compound 15 (-7.80 kcal/mol) and shown greater binding affinity than fluconazole (-7.60 kcal/mol). Docking was performed with protein crystalline structure (PDB ID: 2WEE) of Mycobacterium tuberculosis H37Rv (MTB) stain and among all, compound 5 was exhibited good binding affinity (-6.90 kcal/mol), compared to pyrazinamide (-4.10 kcal/mol). The protein crystalline structure of a mutant androgen receptor (AR) ligand-binding domain (LBD) (PDB file: 1GS4) was tested with compounds 15 and 17 (-7.60 and -8.20 kcal/mol). They were exhibited good binding properties compared to methotrexate (-5.10 kcal/mol). Hence, these novel pyrimidine compounds are as lead compounds as antifungal, antitubercular and cytotoxic agents.

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

Functional, structural and epitopic prediction of hypothetical proteins of Mycobacterium tuberculosis H37Rv: An in silico approach for prioritizing the targets

Gene ◽  
2016 ◽  
Vol 591 (2) ◽  
pp. 442-455 ◽  
Author(s):  
Md. Amran Gazi ◽  
Mohammad Golam Kibria ◽  
Mustafa Mahfuz ◽  
Md. Rezaul Islam ◽  
Prakash Ghosh ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
In Silico ◽  
Tuberculosis H37rv ◽  
Hypothetical Proteins ◽  
Mycobacterium Tuberculosis H37rv

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

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.

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