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

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

European journal of medicinal chemistry (2012-01-06)
Yaşar Dürüst, Hamza Karakuş, Marcel Kaiser, Deniz Tasdemir
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Miltefosine, ≥98% (perchloric acid titration)
Sigma-Aldrich
Podophyllotoxin