Synthesis of 4-amino-5-cyano-2, 6-Disubstituted Pyrimidines as a Potential Antifilarial DNA Topoisomerase II Inhibitors

Author(s): Ashok Kumar , J. K. Saxena , Prem M.S. Chauhan .

Journal Name: Medicinal Chemistry

Volume 4 , Issue 6 , 2008

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Abstract:

A novel series of 4-amino-5-cyano-2, 6-disubstituted pyrimidines have been synthesized and evaluated for their in vitro antifilarial DNA topoisomerase II activity against filarial parasite Setaria Cervi. In particular compounds bearing 4-chloro-phenyl substitutent at position-6, exhibited strong inhibition at 40 μg/mL and 5 μg/mL concentration. The present study based on the biological results obtained, suggests that the nature of substitutent at position-4 in the phenyl ring directly affects DNA topoisomerase II inhibitory activity. Most of the compounds have shown better topoisomerase II inhibitory activity than the standard antifilarial drug (DEC) and the topoisomerase II inhibitors (Novobiocin, Nalidixic acid).

Keywords: Pyrimidine, antifilarial, topoisomerase II, knoevenagel condensation

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Article Details

VOLUME: 4
ISSUE: 6
Year: 2008
Page: [577 - 585]
Pages: 9
DOI: 10.2174/157340608786242115
Price: $58

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