scholarly journals ANTITUBERCULAR ACTIVITY OF SOME NEWER 6-PYRIDAZINONE DERIVATIVES

2011 ◽  
Vol 19 (19) ◽  
pp. 17-23
Author(s):  
Asif HUSAIN ◽  
Aftab AHMAD ◽  
Anil BHANDARI ◽  
Veerma RAM
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Activity ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv ◽  
H37rv Strain ◽  
Pyridazinone Derivatives

Two series of 6-pyridazinone derivatives (17-30) were synthesized and evaluated for antitubercular activities against the Mycobacterium tuberculosis H37Rv strain. The results indicated that among the synthesized compounds, 5-( 4-hydroxy-3-methoxybenzyl}-3-phenyl-1,6-dihydro-6-pyridazinone (23) showed good antitubercular activity. Three more compounds, (18, 25 & 27) were significant in their antitubercular action. The present study reveals the antitubercular potential of 6-pyridazinones.

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.

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 Design and characterisation of piperazine-benzofuran integrated dinitrobenzenesulfonamide as Mycobacterium tuberculosis H37Rv strain inhibitors

2021 ◽  
Vol 36 (1) ◽  
pp. 1751-1759
Author(s):  
Vallabhaneni S. Murthy ◽  
Yasinalli Tamboli ◽  
Vagolu Siva Krishna ◽  
Dharmarajan Sriram ◽  
Siddique Akber Ansari ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv ◽  
H37rv Strain

scholarly journals Potentialy Of Flavonoid Miana (Coleus Atropurpereus) Leaves Estract As Anti Mycobacterium Tuberculosis H37rv Strain And Mdr With Microscopy Observation Drug Susceptibility (Mods)

2018 ◽  
Vol 9 (2) ◽  
Author(s):  
Anita Anita ◽  
Dewi Arisanti ◽  
Andi Fatmawati
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Qualitative Method ◽  
Drug Susceptibility ◽  
Tuberculosis H37rv ◽  
Mycobacterium Tuberculosis H37rv ◽  
Resistant Tuberculosis ◽  
South Sulawesi ◽  
H37rv Strain ◽  
Mdr Tb ◽  
All Diseases

There is high resistance cases for Isoniazid and Rifampin and more famous withMulti-drug resistant tuberculosis (MDR-TB). From data in Makassar, South sulawesishowed 19,2 MDR-TB cases from new TB patient, and more 13,5% resistance cases forfirstline-TB drugs (STR, INH, RIF,and ETH), and >2 resistance for secondline-TBdrugs (OFL,KAN,AMK). Treatment for tuberculosis mostlly not effective because Multidrugresistanttuberculosis (MDR-TB) cases is very high.WHO recomended traditionalmedicine for improvement of healthy in coummunity, preventive and pharmaceuticalpreparation for all diseases. Research in 2013 showed 85,71% that Torajas TB patientin South Sulawesi used traditional medicine such as Miana (Coleus atropurpereus)leaves estract as complement for TB drugs. Our study showed flavonoid component fromqualitative method used sianida (HCl-Mg) from ethanol 96% Miana (Coleusatropurpereus) leaves estract .Qualitative method using Spektrofotometer UV-V showedthe total of flavonoid component from ethanol 96% miana (Coleus atropurpereus) leavesestract is 8,59 mgRE/gram ekstract.. The result showed were at concentrations (10%,20% ,40 % , 60 % ,80 % and 100%) ethanol 96% miana (Coleus atropurpereus) leavesestract were effecttively inhibit Mycobacterium tuberculosis H37RV strain. Were atconcentration (10%, 20% ,40 % dan 60 %) ethanol 96% miana (Coleus atropurpereus)leaves estract were not effecttively inhibit MDR-TB but effecttively were at concentration (80 % and 100%).

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.

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