Vaidyanath Research Training and Diagnostic Center

Kurukshetra, India

Vaidyanath Research Training and Diagnostic Center

Kurukshetra, India

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Kaur K.,M M University | Kumar V.,M M University | Beniwal V.,M M University | Kumar V.,Kurukshetra University | And 3 more authors.
Medicinal Chemistry Research | Year: 2015

In search of novel biologically active azoles, some new (E)-2-(3,5-dimethyl-4-(aryldiazenyl)-1H-pyrazol-1-yl)-4-arylthiazoles 3a-p have been synthesized via Hantzsch thiazole approach under greener, mild and solvent-free conditions. Structures of all compounds were established on the basis of the rigorous elemental analysis and their IR, NMR (1H, 13C), COSY, ROSEY, HSQC and HMBC spectral data. To explore the biological potential, all the synthesized compounds were evaluated for their antimicrobial, antioxidant and UV-mediated DNA damage-protective and photocleavage activity. The results of antimicrobial study revealed that among the series, compounds 3g-l were found active selectively against C. albicans. The compound 3l exhibited twofold high antifungal potential in comparison with amphotericin-B, a standard drug against C. albicans. The compound 3k was found equipotent, and 3g-j displayed half of the potential in reference to the standard drug. In UV-induced DNA damage-protecting and photocleavage study, 3j and 3n were found as the most potent DNA damage-protecting and DNA-photocleaving agents, respectively, at 40 μg concentration. The compounds 3d, 3e, 3g, 3i, 3k, 3m and 3o also displayed a significant level of DNA damage-protective potential, whereas 3l and 3p exhibited appreciable DNA photocleavage activity. In the antioxidant study, all compounds were found inactive. © 2015 Springer Science+Business Media New York.


Kaur K.,M M University | Kumar V.,M M University | Beniwal V.,M M University | Kumar V.,Kurukshetra University | And 3 more authors.
Medicinal Chemistry Research | Year: 2015

In search of new biologically active compounds, some novel (E)-1-aryl-2-(3,5-dimethyl-4-(aryldiazenyl)-1H-pyrazol-1-yl)ethanones 3a-u have been synthesized via solvent-free greener approach. All compounds were characterized on the basis of a combined use of IR, NMR (1H, 13C), mass spectrometry and elemental analyses. In order to establish the position of methyl groups in the compound 3b, 2D NMR (COSY, HSQC and HMBC) spectroscopic technique has also been used. To explore the biological potential, compounds were evaluated for their antimicrobial, antioxidant and UV-mediated DNA damage protective activity. Among the series, six compounds 3b, 3i, 3k, 3l, 3m and 3t were found to exhibit a very good level of antibacterial activity and four compounds 3g, 3o, 3p and 3t were emerged as an efficient class of antifungal agents in reference to the standard drugs, viz ciprofloxacin and amphotericin B, respectively. In studying the UV-mediated DNA damage protective activity, all compounds 3a-u (except 3d) protected the plasmid DNA from the UV damaging effect in which 3e was found to be the most potent DNA-protecting agent which avoids the transformation of the native supercoiled form into an open circular and linear form. In addition, the compounds 3f, 3m and 3t were found to be active in antioxidant screening using DPPH assay. © 2015 Springer Science+Business Media New York.


Kamal R.,Kurukshetra University | Kumar V.,Kurukshetra University | Bhardwaj V.,Kurukshetra University | Kumar V.,Vaidyanath Research Training and Diagnostic Center | Aneja K.R.,Seth Jai Parkash Mukad Lal Institute of Engineering and Technology
Medicinal Chemistry Research | Year: 2015

In the present investigation, ten new 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(4,6-dimethylpyrimidin-2-yl)hydrazine (3a-j) having pyrimidinyl and pyrazolyl moieties were synthesized. Structures of all compounds were confirmed by their spectral and elemental data. Most of the tested compounds were found to be significantly more effective against bacterial strains Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa than the reference drug ciprofloxacin. All the newly synthesized compounds were found to be more potent antifungal agents than reference drug against Candida albicans, whereas except 3e all other compounds also shown good activity against Saccharomyces cerevisiae. © 2014 Springer Science+Business Media.

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