RP-HPLC analysis and in vitro identification of antimycobacterial activity of novel thiosemicarbazides and 1,2,4-triazole derivatives

2015 ◽  
Vol 107 ◽  
pp. 501-511 ◽  
Author(s):  
Jolanta Flieger ◽  
Małgorzata Tatarczak-Michalewska ◽  
Monika Wujec ◽  
Monika Pitucha ◽  
Ryszard Świeboda
Keyword(s):  
Hplc Analysis ◽  
Antimycobacterial Activity ◽  
Triazole Derivatives ◽  
Rp Hplc

scholarly journals New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 6033
Author(s):  
Zbigniew Karczmarzyk ◽  
Marta Swatko-Ossor ◽  
Waldemar Wysocki ◽  
Monika Drozd ◽  
Grazyna Ginalska ◽  
...  
Keyword(s):  
Degrees Of Freedom ◽  
Dipole Moments ◽  
Triazole Ring ◽  
Antimycobacterial Activity ◽  
Docking Studies ◽  
Molecular Structures ◽  
In Vitro Test ◽  
X Ray ◽  
Triazole Derivatives

A series of 1,2,4-triazole derivatives were synthesized and assigned as potential anti-tuberculosis substances. The molecular and crystal structures for the model compounds C1, C12, and C13 were determined using X-ray analysis. The X-ray investigation confirmed the synthesis pathway and the assumed molecular structures for analyzed 1,2,4-triazol-5-thione derivatives. The conformational preferences resulting from rotational degrees of freedom of the 1,2,4-triazole ring substituents were characterized. The lipophilicity (logP) and electronic parameters as the energy of frontier orbitals, dipole moments, NBO net charge distribution on the atoms, and electrostatic potential distribution for all structures were calculated at AM1 and DFT/B3LYP/6-311++G(d,p) level. The in vitro test was done against M. tuberculosis H37Ra, M. phlei, M. smegmatis, and M. timereck. The obtained results clearly confirmed the antituberculosis potential of compound C4, which turned out to be the most active against Mycobacterium H37Ra (MIC = 0.976 μg/mL), Mycobaterium pheli (MIC = 7.81 μg/mL) and Mycobacerium timereck (62.6 μg/mL). Satisfactory results were obtained with compounds C8, C11, C14 versus Myc. H37Ra, Myc. pheli, Myc. timereck (MIC = 31.25−62.5 μg/mL). The molecular docking studies were carried out for all investigated compounds using the Mycobacterium tuberculosis cytochrome P450 CYP121 enzyme as molecular a target connected with antimycobacterial activity.

The medicinal herb Spatholobus suberectus with promising in vitro antioxidant and anti-inflammatory potentials and its phytochemical characterization by RP-HPLC analysis

2017 ◽  
Vol 42 (2) ◽  
pp. e12480 ◽  
Author(s):  
Md. Mohibbullah ◽  
Ye Jin Lee ◽  
Hyun-Jin Park ◽  
Sung Kew Kim ◽  
Jin-Sook Kang ◽  
...  
Keyword(s):  
Hplc Analysis ◽  
Medicinal Herb ◽  
Rp Hplc ◽  
Spatholobus Suberectus ◽  
Anti Inflammatory

RP-HPLC analysis of withanolides in the flowers, leaves, and roots ofWithania somnifera

2010 ◽  
Vol 22 (3) ◽  
pp. 473-480 ◽  
Author(s):  
N. W. Ali ◽  
S. Abouzid ◽  
A. Nasib ◽  
S. Khan ◽  
J. Qureshi ◽  
...  
Keyword(s):  
Hplc Analysis ◽  
Rp Hplc ◽  
Leaves And Roots

RP-HPLC ANALYSIS OF CARBONYL COMPOUNDS IN SOME INDOOR AIR SAMPLES IN A FACULTY FROM CLUJ-NAPOCA

2013 ◽  
Vol 12 (2) ◽  
pp. 219-225
Author(s):  
Carmen Roba ◽  
Cristina Rosu ◽  
Iulia Neamtiu ◽  
Eugen Gurzau
Keyword(s):  
Indoor Air ◽  
Carbonyl Compounds ◽  
Hplc Analysis ◽  
Air Samples ◽  
Rp Hplc

Extraction, Chemical Composition, Antioxidant Property and In vitro Anticancer Activity of Silymarin from Silybum Marianum On Kb and A549 Cell Lines

2020 ◽  
Vol 17 ◽  
Author(s):  
Mojgan Azadpour ◽  
Mohammad Mehdi Farajollahi ◽  
Ali Mohammad Varzi ◽  
Pejman Hashemzadeh ◽  
Hossein Mahmoudvand ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
A549 Cell ◽  
Hplc Analysis ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Silybum Marianum ◽  
Stable Free Radical

Introduction: This study aimed to evaluate the antioxidant property of silymarin (SM) extracted from the seed of Silybum marianum and its anticancer activity on KB and A549 cell lines following 24, 48, and 72 h of treatment. Methods: Ten grams of powdered S. marianum seeds were defatted using n-hexane for 6 hours and then extracted by methanol. The silymarin extracted of extraction components The extracted components of silymarin were measured by spectrophotometric assay and HPLC analysis. 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, phenol content, total flavonoid content, and total antioxidant capacity were measured to detect the antioxidant properties of SM. The anticancer activity of the SM on cell lines evaluated by MTT. Results: In HPLC analysis, more than 50% of the peaks were related to silibin A and B. SM was reducedDPPH (the stable free radical) with a 50% inhibitory concentration (IC50) of 6.56 μg/ ml in comparison with butylated hydroxyl toluene (BHT), which indicated an IC50 of ~3.9 μg/ ml.The cytotoxicity effect of SM on the cell lines was studied by MTT assay. The cytotoxicity effect of the extracted silymarin on KB and A549 cell lines was observed up to 80 and 70% at 156 and 78 µg/ml, respectively. The IC50 value of the extracted SM on KB and A549 cell lines after 24 hours of treatment was seen at 555 and 511 µg/ml, respectively. Conclusion: Due to the good antioxidant and anticancer properties of the isolated silymarin, its use as an anticancer drug is suggested.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

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