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

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

Volume: 4 Issue: 6

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

Affiliation:

Keywords: Pyrimidine, antifilarial, topoisomerase II, knoevenagel condensation

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).

Cite this article as:

Kumar Ashok, Saxena K. J. and Chauhan M.S. Prem, Synthesis of 4-amino-5-cyano-2, 6-Disubstituted Pyrimidines as a Potential Antifilarial DNA Topoisomerase II Inhibitors, Medicinal Chemistry 2008; 4 (6) . https://dx.doi.org/10.2174/157340608786242115