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Solid phase synthesis of quinolones.

S K Srivastava1, W Haq, P K Murthy

  • 1Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, India.

Bioorganic & Medicinal Chemistry Letters
|August 18, 1999
PubMed
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New quinolone derivatives were synthesized and tested for antifilarial activity. Compounds 5, 7a-d showed in vitro activity against Brugia malayi, indicating potential as antifilarial agents.

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Organic Synthesis

Background:

  • Filariasis remains a significant global health concern, necessitating novel therapeutic agents.
  • Quinolone derivatives have demonstrated diverse biological activities, including antiparasitic effects.

Purpose of the Study:

  • To synthesize novel ethyl 6-carboxyquinol-4(1H)-one-3-carboxylate and N-substituted 6-carboxyquinol-4(1H)-one-3-carboxamide derivatives.
  • To evaluate the in vitro antifilarial activity of these synthesized compounds against Brugia malayi.

Main Methods:

  • Solid-phase synthesis techniques were employed for the preparation of target compounds.
  • In vitro assays were conducted to assess the efficacy of compounds against Brugia malayi.

Main Results:

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  • Successful synthesis of ethyl 6-carboxyquinol-4(1H)-one-3-carboxylate (5) and N-substituted 6-carboxyquinol-4(1H)-one-3-carboxamides (7a-d).
  • Compounds 5, 7a-d exhibited significant in vitro activity against Brugia malayi.

Conclusions:

  • The synthesized quinolone derivatives show promise as potential candidates for antifilarial drug development.
  • Further investigation is warranted to explore their therapeutic potential and mechanism of action.