“Whoa! It’s like Spotify but for academic articles.”

Instant Access to Thousands of Journals for just $40/month

Try 2 weeks free now

In vivo antimalarial activity of novel 2-hydroxy-3-anilino-1,4-naphthoquinones obtained by epoxide ring-opening reaction

1,4-Naphthoquinones are a class of compounds broadly studied in organic synthesis, medicinal chemistry and natural products chemistry. 1 Within these studies, the antimalarial activity has been widely reported for several 1,4-naphthoquinones. 2 The antiparasitic activity of the quinones is related to several mechanisms such as the competitive inhibition of the cytochrome bc1 complex, generation of reactive oxygen species, enzymatic inhibition (e.g., glutathione reductase, dihydroorotate dehydrogenase and glycerol glyceraldehyde-3-phosphate dehydrogenase) alkylation of biomolecules, depletion of glutathione, among others. 3 </P>Lawsone derivatives containing the 2-hydroxy-1,4-naphthoquinone scaffold are highly explored for the development of novel antiparasitics. Atovaquone, parvaquone and buparvaquone are 3-substituted-2-hydroxy-1,4-naphthoquinones clinically applied as antimalarial (atovaquone) and antipneumocystic (parvaquone and buparvaquone) agents, which exemplifies the potentiality of such scaffold in the development of novel drugs. Additionally, some studies indicate the potential application of natural or synthetic 2-amino-1,4-naphthoquinones and 2-amino-1,2-naphthoquinones as antiplasmodial agents. 4 </P>Despite the pharmacological relevance of aminated and hydroxylated naphthoquinoidal derivatives and the wide structural diversity of 1,4-naphthoquinones, 2-amino-3-hydroxy-1,4-naphthoquinone is an uncommon structural fragment only observed in few examples of natural products and bioactive compounds. 5 Recently 2-(4-phenylpiperazinyl)-3-hydroxy-1,4-naphthoquinone 1 , 6 which can be seen as a ring bioisostere of atovaquone, was shown to have inhibitory effects against http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Letters Elsevier
Loading next page...

You’re reading a free preview. Subscribe to read the entire article.

DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy unlimited access and
personalized recommendations from
over 12 million articles from more than
10,000 peer-reviewed journals.

All for just $40/month

Try 2 weeks free now

Explore the DeepDyve Library

How DeepDyve Works

Spend time researching, not time worrying you’re buying articles that might not be useful.

Unlimited reading

Read as many articles as you need. Full articles with original layout, charts and figures. Read online, from anywhere.

Stay up to date

Keep up with your field with Personalized Recommendations and Follow Journals to get automatic updates.

Organize your research

It’s easy to organize your research with our built-in tools.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from Springer, Elsevier, Nature, IEEE, Wiley-Blackwell and more.

All the latest content is available, no embargo periods.

See the journals in your area

Simple and Affordable Pricing

14-day free trial. Cancel anytime, with a 30-day money-back guarantee.

Monthly Plan

  • Read unlimited articles
  • Personalized recommendations
  • Print 20 pages per month
  • 20% off on PDF purchases
  • Organize your research
  • Get updates on your journals and topic searches


Best Deal — 25% off

Annual Plan

  • All the features of the Professional Plan, but for 25% off!
  • For the normal price of 10 articles elsewhere, you get one full year of unlimited access to articles.

billed annually