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.
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Authors | Yaşar Dürüst, Hamza Karakuş, Marcel Kaiser, Deniz Tasdemir |
Journal | European journal of medicinal chemistry
(Eur J Med Chem)
Vol. 48
Pg. 296-304
(Feb 2012)
ISSN: 1768-3254 [Electronic] France |
PMID | 22217867
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2011 Elsevier Masson SAS. All rights reserved. |
Chemical References |
- Antiprotozoal Agents
- Oxadiazoles
- Pyrroles
- Triazoles
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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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