scholarly journals Tenuazonic acid: a promising antitubercular principle from Alternaria alternate

2011 ◽  
Vol 2 (1) ◽  
pp. 17 ◽  
Author(s):  
Visalakchi Sonaimuthu ◽  
Swati Parihar ◽  
Jay Prakash Thakur ◽  
Suaib Luqman ◽  
Dharmendra Saikia ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Alternaria Alternata ◽  
Active Metabolite ◽  
Antitubercular Activity ◽  
Model System ◽  
Human Erythrocytes ◽  
Tenuazonic Acid ◽  
Fungal Metabolite ◽  
Osmotic Hemolysis ◽  
Alternaria Alternate

Bioactivity guided isolation of dichloromethane extract of <em>Alternaria alternata</em> identified tenuazonic acid (1) as potentially active against <em>Mycobacterium tuberculosis</em> H37Rv, MIC at 250 μg/mL concentration. This active metabolite 1, was also evaluated for osmotic hemolysis using the erythrocyte as a model system. It was observed that this fungal metabolite showing antitubercular activity exhibited concentration dependent toxicity to human erythrocytes.

Elemental analysis of human erythrocytes

1989 ◽  
Vol 47 ◽  
pp. 242-243
Author(s):  
S. A. Livesey ◽  
A. A. del Campo ◽  
E. S. Griffey ◽  
D. Ohlmer ◽  
T. Schifani ◽  
...  
Keyword(s):  
Sample Preparation ◽  
Elemental Analysis ◽  
Human Erythrocyte ◽  
Spectroscopic Analysis ◽  
Model System ◽  
Human Erythrocytes ◽  
List Type ◽  
Chemical Fixation ◽  
Ethanol Dehydration ◽  
Lowicryl K4m

The aim of this study is to compare methods of sample preparation for elemental analysis. The model system which is used is the human erythrocyte. Energy dispersive spectroscopic analysis has been previously reported for cryofixed and cryosectioned erythrocytes. Such work represents the reference point for this study. The use of plastic embedded samples for elemental analysis has also been documented. The work which is presented here is based on human erythrocytes which have been either chemically fixed and embedded or cryofixed and subsequently processed by a variety of techniques which culminated in plastic embedded samples.Heparinized and washed erythrocytes were prepared by the following methods for this study :(1). Chemical fixation in 4% paraformaldehyde/0.25% glutaraldehyde/0.2 M sucrose in 0.1 M Na cacodylate, pH 7.3 for 30 min, followed by ethanol dehydration, infiltration and embedding in Lowicryl K4M at -20° C.

Design, Synthesis and Antitubercular Evaluation of New Benzimidazole Scaffolds

2021 ◽  
Vol 18 (4) ◽  
pp. 375-383
Author(s):  
Smriti Yadav ◽  
Bharath Kumar Inturi ◽  
Shrinidhi B.R ◽  
Pooja H.J ◽  
Neenu Ganesh ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Cell Lines ◽  
Normal Cell ◽  
Acyl Carrier Protein ◽  
Antitubercular Activity ◽  
Resistance Mechanisms ◽  
Docking Studies ◽  
Chemical Library ◽  
Activity Data ◽  
Mycobacterium Tuberculosis H37rv

Background: To overcome one of the resistance mechanisms of Isoniazid (INH), there is a need for an antitubercular agent that can inhibit InhA enzyme by circumventing the formation of INH-NAD+ adduct. Objective: The objective of the study is the development of novel antitubercular agents that target Mycobacterium tuberculosis InhA (Enoyl Acyl Carrier Protein Reductase). Methods: A small-molecule chemical library was used for the identification of the novel InhA inhibitors using primary screening and molecular docking studies followed by the scaffold hopping approach. The designed molecules, 2-(2-(hydroxymethyl)-1H- benzo[d] imidazole-1-yl)- N- substituted acetamides were synthesized by reacting (1H- benzo[d]imidazole -2-yl)methanol with appropriate 2-chloro-N-substituted acetamides / dialkylamino carbonyl chlorides respectively in good yields (42-65%). The antitubercular activity of synthesized compounds was determined by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv strain. The selected compounds were screened for cytotoxicity on normal cell lines. Results: The antitubercular activity data revealed that the 4-chlorophenyl substituted derivative (3b) showed good MIC value at 6.25 μg/mL and, dimethylacetamide substituted derivative (3i) showed MIC at 25 μg/mL among the tested compounds. The substitution of dimethylacetamide (3i) group on the 1st position of benzimidazole has good antitubercular activity (25μg/mL) in comparison to the diethyl acetamide group (3j, 100μg/mL). Conclusion: The antitubercular activity data indicated that the tested compounds exhibited well to moderate inhibition of the H37Rv strains. The compounds (3b) with electronegative substitution on the phenyl moiety exhibited better antitubercular activity than that of the other substitutions. The active compounds have displayed a good safety profile on normal cell lines.

Function of glycerol as a protectant against osmotic hemolysis of human erythrocytes

Cryobiology ◽  
1989 ◽  
Vol 26 (6) ◽  
pp. 579
Author(s):  
D.Y. Gag ◽  
J.A. Kornblatt ◽  
S. Lin
Keyword(s):  
Human Erythrocytes ◽  
Osmotic Hemolysis

Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis

2011 ◽  
Vol 21 (24) ◽  
pp. 7273-7276 ◽  
Author(s):  
Poovan Shanmugavelan ◽  
Sangaraiah Nagarajan ◽  
Murugan Sathishkumar ◽  
Alagusundaram Ponnuswamy ◽  
Perumal Yogeeswari ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity ◽  
Efficient Synthesis

scholarly journals Structure-Based Drug Design and Characterization of Sulfonyl-Piperazine Benzothiazinone Inhibitors of DprE1 from Mycobacterium tuberculosis

2018 ◽  
Vol 62 (10) ◽  
Author(s):  
Jérémie Piton ◽  
Anthony Vocat ◽  
Andréanne Lupien ◽  
Caroline S. Foo ◽  
Olga Riabova ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Drug Design ◽  
Antitubercular Activity ◽  
Cysteine Residue ◽  
Drug Candidate ◽  
Structure Based Drug Design ◽  
Content Type ◽  
Active Site Cysteine ◽  
Covalent Adducts

ABSTRACT Macozinone (MCZ) is a tuberculosis (TB) drug candidate that specifically targets the essential flavoenzyme DprE1, thereby blocking synthesis of the cell wall precursor decaprenyl phosphoarabinose (DPA) and provoking lysis of Mycobacterium tuberculosis. As part of the MCZ backup program, we exploited structure-guided drug design to produce a new series of sulfone-containing derivatives, 2-sulfonylpiperazin 8-nitro 6-trifluoromethyl 1,3-benzothiazin-4-one, or sPBTZ. These compounds are less active than MCZ but have a better solubility profile, and some derivatives display enhanced stability in microsomal assays. DprE1 was efficiently inhibited by sPBTZ, and covalent adducts with the active-site cysteine residue (C387) were formed. However, despite the H-bonding potential of the sulfone group, no additional bonds were seen in the crystal structure of the sPBTZ-DprE1 complex with compound 11326127 compared to MCZ. Compound 11626091, the most advanced sPBTZ, displayed good antitubercular activity in the murine model of chronic TB but was less effective than MCZ. Nonetheless, further testing of this MCZ backup compound is warranted as part of combination treatment with other TB drugs.

SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW 1,3,4- OXADIAZOLES, 1,2,4-TRIAZOLES AND 1,3,4-THIADIAZOLES

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (06) ◽  
pp. 18-23
Author(s):  
U. V. Laddi ◽  
◽  
S. R. Desai
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity ◽  
Tuberculosis H37rv ◽  
Research Centre ◽  
Methyl Ethyl ◽  
Rhizoctonia Bataticola ◽  
Mycobacterium Tuberculosis H37rv ◽  
H37rv Strain

Some new 5-[(((α-phenyl/methyl)benzylidene)amino)oxy]methyl/ethyl-2-[4-(substituted aryl)/allyl)] amino-1,3,4-oxadiazoles (4a-p), 3-[(((α-phenyl/methyl)- benzylidene) amino)oxy]methyl/ethyl-4-(4- substitutedaryl)/allyl-5-mercapto-1,2,4-triazoles (5a-p) and 5-[(((α-phenyl/methyl)-benzylidene)amino) oxy]- methyl/ethyl-2-[4-(substituted aryl)/allyl)]amino-1,3,4-thiadiazoles (6a-p) were prepared starting from α/β-[((α-(phenyl/methyl)benzylidene)amino)oxy acetic/propionic acid hydrazides (1a-d). The structures of all the compounds have been established by elemental and spectral (IR, 1HNMR and mass) analysis. All the newly synthesised compounds have been screened for their antimicrobial activity against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Rhizoctonia bataticola. Some of the newly synthesised compounds have been evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv strain by BACTEC radiometric system at Southern Research Institute, Birmingham, AL and Frederick Research Centre, Frederick, MD. Significant antimicrobial activity is observed against Escherichia coli and Rhizoctonia bataticola. A few compounds also exhibited interesting antitubercular activity against Mycobacterium tuberculosis H37Rv strain.

Synthesis and in vitro antitubercular activity of pyridine analouges against the resistant Mycobacterium tuberculosis

2020 ◽  
Vol 102 ◽  
pp. 104099
Author(s):  
Harun Patel ◽  
Kavita Chaudhari ◽  
Pritam Jain ◽  
Sanjay Surana
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity

scholarly journals Synthesis and Preliminary Evaluation of Benzofuran-Oxadiazole Conjugates as Potential Antitubercular Agents

2019 ◽  
Vol 31 (4) ◽  
pp. 965-970 ◽  
Author(s):  
Veerabhadrayya S. Negalurmath ◽  
Obelannavar Kotresh ◽  
Mahantesha Basanagouda
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Spectral Data ◽  
13C Nmr ◽  
Antitubercular Activity ◽  
Preliminary Evaluation ◽  
Antitubercular Agents ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Mycobacterium Tuberculosis H37rv ◽  
Mycobacterium Phlei

In the present study, a series of benzofuran-oxadiazole conjugates 7(a-o) was designed, synthesized and characterized through IR, 1H NMR, 13C NMR and mass spectral data. All the compounds were screened for preliminary antitubercular activity against Mycobacterium phlei and Mycobacterium tuberculosis H37RV. Among all the target compounds, the compound possessing chlorine (7k, MIC 1.56 μg/mL) and bromine (7m, MIC 1.56 μg/mL) on 6th position of benzofuran showed highest activity against Mycobacterium phlei. Whereas, bromine on either 5th position (7l, MIC 3.125 μg/mL) or 6th position (7m MIC 3.125 μg/mL) on benzofuran exhibited highest activity for Mycobacterium tuberculosis (H37 RV).

In vitro Antitubercular Activity of Dihydropyridine-Dicarboxamide and Pyrazole Derivatives against Mycobacterium tuberculosis

2019 ◽  
pp. 102
Author(s):  
Sushil Kumar Upadhyay ◽  
Raj Singh ◽  
Parveen Kumar ◽  
Manoj Singh ◽  
Mukesh Yadav ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity ◽  
Pyrazole Derivatives
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