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Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles.

Abstract
1,2,4-Oxadiazole and 1,2,3-triazole containing heterocyclic compounds continue to gain interest in synthesis of chemical entities and exhibit various biological activities as anti-protozoal and anti-cancer agents. By using the principle of bioisosterism, a series of novel oxadiazolyl pyrrolo triazole diones; namely, (3aS,6aR)-1-((3-(4-substituted phenyl)-1,2,4-oxadiazol-5-yl)methyl)-5-phenyl-1,6a-dihydropyrrolo[3,4-d][1,2,3] triazole-4,6(3aH,5H)-diones (5a-k) was designed and synthesized by the 1,3-dipolar cycloaddition reaction of novel 5-azidomethyl 3-aryl substituted 1,2,4-oxadiazoles (4a-k) with N-phenyl maleimide. The structures of all the cycloadducts were elucidated by means of spectroscopic methods and physical characteristics. The in vitro anti-protozoal and cytotoxic activities of these novel heterocyclic compounds were investigated.
AuthorsYaşar Dürüst, Hamza Karakuş, Marcel Kaiser, Deniz Tasdemir
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 48 Pg. 296-304 (Feb 2012) ISSN: 1768-3254 [Electronic] France
PMID22217867 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2011 Elsevier Masson SAS. All rights reserved.
Chemical References
  • Antiprotozoal Agents
  • Oxadiazoles
  • Pyrroles
  • Triazoles
Topics
  • Animals
  • Antiprotozoal Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line
  • Eukaryota (drug effects, growth & development)
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Oxadiazoles (chemical synthesis, chemistry, pharmacology)
  • Protozoan Infections (drug therapy)
  • Pyrroles (chemical synthesis, chemistry, pharmacology)
  • Rats
  • Spectrometry, Mass, Electrospray Ionization
  • Spectroscopy, Fourier Transform Infrared
  • Structure-Activity Relationship
  • Triazoles (chemical synthesis, chemistry, pharmacology)

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