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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine
Sham M Sondhi1, Reshma Rani, Partha Roy
1Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttaranchal, India.
Abstract:
Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via microwave irradiation in good yields. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50mg/kg p.o. compounds 3a (36.6%), 3d (32%), 4d (31.0%) and 4e (33.8%) exhibited good anti-inflammatory activity, comparable to standard drug ibuprofen which showed 39% activity at 50mg/kg p.o.
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