Synthesis and Characterization of Substituted Ethyl 2-(1-aminocyclobutyl)- 5-(benzoyloxy)-6-hydroxypyrimidine-4-carboxylate Derivatives as Antioxidant Agents

Authors: Asha, D.; Malviya, Manish; Chandrappa, S.; Sadashiva, C. T.; Vinaya, K.; Prasanna, D. S.; Rangappa, K. S.

Source: Letters in Drug Design & Discovery, Volume 6, Number 8, December 2009 , pp. 637-643(7)

Publisher: Bentham Science Publishers

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Abstract:

A series of novel ethyl 2-(1-aminocyclobutyl)-5-(benzoyloxy)-6-hydroxy-pyrimidine-4-carboxylate derivatives 8(a-i) were synthesized by nucleophilic substitution reaction of ethyl 2-(1-aminocyclobutyl)-5-(benzoyloxy)-6-hydroxypyrimidine- 4-carboxylate (7) with different substituted aliphatic/aromatic sulfonyl chlorides (R-SO2-Cl). All the synthesized compounds were characterized by IR, 1H NMR and LC/MS analysis. The synthesized compounds were evaluated for their antioxidant activity by diphenylpicrylhydrazyl (DPPH) assay and also by hydroxy radical induced DNA strand scission assay. Among the synthesized compounds 8c, 8f and 8i showed promising antioxidant activity.

Keywords: Benzyl 1-cyanocyclobutylcarbamate; Pyrimidine; Hydroxy radical; DPPH Assay; Antioxidant

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018009789353509

Publication date: 2009-12-01

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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