Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents

Harmeet S. Sandhu, Sameer Sapra, Mukesh Gupta, Kunal Nepali, Raju Gautam, Sunil Yadav, Raj Kumar, Sanjay M. Jachak, Manoj Chugh, Manish K. Gupta, Om P. Suri, K. L. Dhar

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30 引文 斯高帕斯(Scopus)

摘要

A series of arylidene analogues of Meldrum's acid were synthesized and evaluated for in vitro antimalarial and antioxidant activities for the first time. The influence of various physico-chemical parameters such as dielectric constant (), donor number (DN), acceptor number (AN), hydrogen bond donor (HBD), hydrogen bond acceptor (HBA), and solubilizing power of the solvents on Meldrum's acid anion generation and thus on promoting the Knoevenagel condensation of Meldrum's acid with aryl aldehydes has been discussed. Five compounds 9l, 9m, 9n, 9r, and 9s were found to be most active against Plasmodium falciparum with IC50 values in the range of 9.68-16.11 μM. Compound 9l exhibited the most potent antimalarial activity (IC50 9.68 μM). The compounds were also found to possess antioxidant activity when tested against DPPH and ABTS free radicals.
原文英語
頁(從 - 到)5626-5633
頁數8
期刊Bioorganic and Medicinal Chemistry
18
發行號15
DOIs
出版狀態已發佈 - 八月 1 2010
對外發佈

ASJC Scopus subject areas

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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