SYNTHESIS AND BIOEVALUATION OF KETOCONAZOLE THIOSEMICARBAZONE ANALOGUES
AbstractKetoconazole (KTZ) is a synthetic antifungal drug used to prevent and treat fungal infections, especially in immunocompromised patients such as those with AIDS. Resistance to ketoconazole has been observed in a number of clinical fungal isolates, including C. albicans. Thus new effective agents with less toxicity against fungal infection are urgently required. With this view, ketoconazole thiosemicarbazone analogues (Compounds 1-10) were synthesized wherein condensation of different thiosemicarbazides substituted by different cyclic and aromatic amines with the KTZ was done. Investigation of in-vitro antifungal activity of compounds was done by broth microdilution assay method against five pathogenic fungi Aspergillus niger, Candida albicans, Candida krusei, Candida glabrata and Candida tropicalis. Ketoconazole was used as reference for inhibitory activity against fungi. All the compounds were found potent antifungal agents, while compounds 8, 9 and 10 exhibited excellent in-vitro antifungal activity showing importance of halogenated compounds
Article Information
18
3157-3160
458
1571
English
Ijpsr
T. K. Agrawal and Y. Murti*
Assistant Professor (Pharmaceutical Chemistry), Institute of Pharmaceutical Research, GLA University, Mathura, 17, Km Stone, National Highway #2, Delhi-Mathura Road, P.O. Chaumuha, Mathura-281406, Uttar Pradesh, India
09 August, 2011
September, 2011
10 November, 2011
http://dx.doi.org/10.13040/IJPSR.0975-8232.2(12).3157-60
01 December, 2011
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