DESIGN, SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL EVALUATION OF NEW PYRAZOLINE-5-ONES
Krishna Naik
1. Sri Krishnadevaraya Univerisity, Anantapur, Andhra Pradesh, India. 2. ICFAI Foundation for Higher Education, Hyderabad, Andhra Pradesh, India.
Keywords: Phenyl hydrdrazones, Synthesis, Structural elucidation, Antibacterial activity, Antifungal activity.
Abstract

Purpose: To synthesise, charecterise phenyl hydrazones namely, {4-[3-methyl-5-oxo-4-(phenyl hydrazono)-4,5-dihydro-pyrazol-1-yl]-phenoxy}-acetic acid N|-(4-substituted-thiazole-2-yl)-hydrazide VII and to evaluate the antibacrial activity. Methods: The synthesis of title compounds has been schemed elaborately and the structures of the compounds were established by elemental analysis, IR, 1H NMR and mass spectra. The antibacterial activity of the title compounds were evaluated against Staphylococcus aureus NCCS 2079 and Bacillus cereus NCCS 2106, Escherichia coli NCCS 265 and Pseudomonas aeruginosa NCCS 2200 and antifungal activity evaluated against Aspergillus niger NCCS 1196, Candida albicans NCCS 2106 by disk diffusion method. Results: The screened data reveal that the studied phenyl hydrazones under study exhibited promising antimicrobial activity against all the tested microbes. The antimicrobial activity of title compounds were compared with that of standadards. The title compounds with p-nitrophenyl, p-chlorophenyl, p-bromophenyl were more active agaist bacteria, where as the compounds with substituents namely phenyl, p-tolyl, p-anisyl, p-hydroxyphenyl, p-nitrophenyl were more active against fungi than the other compounds under investigation. Conclusion: Among the ten novel phenyl hydrazones synthesised {4-[3-methyl-5-oxo-4-(phenyl hydrazono)-4,5-dihydro-pyrazol-1-yl]-phenoxy}-acetic acid N|-(4-(4-nitro-phenyl)-thiazole-2-yl)-hydrazide was found the most active than the others. The other compounds demonstrated moderate activity against the tested microorganisms.

Article Information

Identifiers and Pagination:
Year:2013
Volume:5
First Page:16
Last Page:26
Publisher Id:JAppPharm (2013 ). 5. 16-26
Article History:
Received:October 27, 2012
Accepted:December 14, 2012
Collection year:2012
First Published:January 1, 2013


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Prof. Dr. Cornelia M. Keck (Philipps-Universität Marburg)
Marburg, Germany

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Welcome to the research group of Prof. Dr. Cornelia M. Keck in Marburg. Cornelia M. Keck is a pharmacist and obtained her PhD in 2006 from the Freie Universität (FU) in Berlin. In 2009 she was appointed as Adjunct Professor for Pharmaceutical and Nutritional Nanotechnology at the University Putra Malaysia (UPM) and in 2011 she obtained her Venia legendi (Habilitation) at the Freie Universität Berlin and was appointed as a Professor for Pharmacology and Pharmaceutics at the University of Applied Sciences Kaiserslautern. Since 2016 she is Professor of Pharmaceutics and Biopharmaceutics at the Philipps-Universität Marburg. Her field of research is the development and characterization of innovative nanocarriers for improved delivery of poorly soluble actives for healthcare and cosmetics. Prof. Keck is executive board member of the German Association of Nanotechnology (Deutscher Verband Nanotechnologie), Vize-chairman of the unit „Dermocosmetics“ at the German Society of Dermopharmacy, active member in many pharmaceutical societies and member of the BfR Committee for Cosmetics at the Federal Institute for Risk Assessment (BfR).

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